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Lapatinib (GW572016) Inibitore di EGFR/HER2

Name: Lapatinib (GW572016)
Brand: Selleck Chemicals
SKU: S2111
Rating: 5 (490 reviews)

N. Cat.S2111

Lapatinib è un potente inibitore di EGFR ed ErbB2 con IC50 di 10,8 e 9,2 nM in saggi senza cellule, rispettivamente. Lapatinib induce ferroptosis e morte cellulare autofagica.

Lapatinib (GW572016) EGFR inibitore Chemical Structure

Struttura chimica

Peso molecolare: 581.06

Vai a

Controllo Qualità

Lotto: Purezza: 99.95%

99.95

Target correlati	VEGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Altro EGFR Inibitori	Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) Genistein

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	PMID
LB2241-RCC	Growth Inhibition Assay			IC50=1.15403 μM	SANGER
TE-9	Growth Inhibition Assay			IC50=0.74453 μM	SANGER
A388	Growth Inhibition Assay			IC50=0.72258 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=0.49057 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=0.44874 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=0.24654 μM	SANGER
BT-474	Growth Inhibition Assay			IC50=0.21315 μM	SANGER
DSH1	Growth Inhibition Assay			IC50=0.09396 μM	SANGER
ECC12	Growth Inhibition Assay			IC50=0.09231 μM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=0.0574 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=0.05326 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=0.02544 μM	SANGER
LB996-RCC	Growth Inhibition Assay			IC50=1.36228 μM	SANGER
LC-1F	Growth Inhibition Assay			IC50=1.38244 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=1.55201 μM	SANGER
A253	Growth Inhibition Assay			IC50=1.97335 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=1.99199 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=2.0483 μM	SANGER
RL95-2	Growth Inhibition Assay			IC50=3.1567 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=3.40041 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=3.46975 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=3.54501 μM	SANGER
TE-10	Growth Inhibition Assay			IC50=3.55356 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=4.0373 μM	SANGER
TK10	Growth Inhibition Assay			IC50=4.16522 μM	SANGER
UACC-812	Growth Inhibition Assay			IC50=4.56153 μM	SANGER
SW962	Growth Inhibition Assay			IC50=5.02159 μM	SANGER
SW954	Growth Inhibition Assay			IC50=5.39245 μM	SANGER
COLO-668	Growth Inhibition Assay			IC50=5.72667 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=5.80046 μM	SANGER
NB5	Growth Inhibition Assay			IC50=6.21001 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=6.26561 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=6.43694 μM	SANGER
GI-1	Growth Inhibition Assay			IC50=6.51682 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=7.07183 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=7.22744 μM	SANGER
EVSA-T	Growth Inhibition Assay			IC50=7.42811 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=7.48894 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=7.76159 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=9.11675 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=9.47395 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=9.5742 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=9.66287 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=9.96307 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=9.98291 μM	SANGER
TE-15	Growth Inhibition Assay			IC50=10.245 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=10.2565 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=10.623 μM	SANGER
RCC10RGB	Growth Inhibition Assay			IC50=10.961 μM	SANGER
KNS-42	Growth Inhibition Assay			IC50=11.7255 μM	SANGER
LB771-HNC	Growth Inhibition Assay			IC50=12.1712 μM	SANGER
SR	Growth Inhibition Assay			IC50=12.2064 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=12.8985 μM	SANGER
ES6	Growth Inhibition Assay			IC50=13.078 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=13.2577 μM	SANGER
D-392MG	Growth Inhibition Assay			IC50=13.6428 μM	SANGER
NB7	Growth Inhibition Assay			IC50=14.2374 μM	SANGER
SK-LMS-1	Growth Inhibition Assay			IC50=14.5145 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=14.7889 μM	SANGER
CA46	Growth Inhibition Assay			IC50=15.0586 μM	SANGER
IST-SL2	Growth Inhibition Assay			IC50=15.1901 μM	SANGER
BC-1	Growth Inhibition Assay			IC50=15.3314 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=15.8173 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=16.0924 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=16.7313 μM	SANGER
LB647-SCLC	Growth Inhibition Assay			IC50=16.9372 μM	SANGER
NCI-H1694	Growth Inhibition Assay			IC50=17.1529 μM	SANGER
NCI-H322M	Growth Inhibition Assay			IC50=17.4366 μM	SANGER
ES7	Growth Inhibition Assay			IC50=18.3914 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=18.4386 μM	SANGER
SF268	Growth Inhibition Assay			IC50=18.7409 μM	SANGER
RPMI-8402	Growth Inhibition Assay			IC50=19.0742 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=20.2344 μM	SANGER
A101D	Growth Inhibition Assay			IC50=20.8587 μM	SANGER
MRK-nu-1	Growth Inhibition Assay			IC50=20.913 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=21.038 μM	SANGER
NALM-6	Growth Inhibition Assay			IC50=21.1967 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=21.4813 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=22.1402 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=22.2149 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=22.3965 μM	SANGER
SKM-1	Growth Inhibition Assay			IC50=22.7351 μM	SANGER
DMS-153	Growth Inhibition Assay			IC50=23.4204 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay			IC50=23.5452 μM	SANGER
LP-1	Growth Inhibition Assay			IC50=23.8097 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=24.292 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=25.2036 μM	SANGER
U-698-M	Growth Inhibition Assay			IC50=25.2503 μM	SANGER
HC-1	Growth Inhibition Assay			IC50=25.6418 μM	SANGER
HCC2157	Growth Inhibition Assay			IC50=25.673 μM	SANGER
MOLT-4	Growth Inhibition Assay			IC50=26.273 μM	SANGER
LS-411N	Growth Inhibition Assay			IC50=26.3369 μM	SANGER
Becker	Growth Inhibition Assay			IC50=26.5181 μM	SANGER
NCI-H23	Growth Inhibition Assay			IC50=26.7575 μM	SANGER
IST-SL1	Growth Inhibition Assay			IC50=27.3867 μM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=27.4566 μM	SANGER
RKO	Growth Inhibition Assay			IC50=28.1446 μM	SANGER
TE-441-T	Growth Inhibition Assay			IC50=28.789 μM	SANGER
EW-24	Growth Inhibition Assay			IC50=29.1259 μM	SANGER
no-10	Growth Inhibition Assay			IC50=29.1631 μM	SANGER
D-542MG	Growth Inhibition Assay			IC50=29.9221 μM	SANGER
ST486	Growth Inhibition Assay			IC50=30.6451 μM	SANGER
KURAMOCHI	Growth Inhibition Assay			IC50=30.8057 μM	SANGER
ES8	Growth Inhibition Assay			IC50=31.5972 μM	SANGER
BL-41	Growth Inhibition Assay			IC50=32.1054 μM	SANGER
NB6	Growth Inhibition Assay			IC50=32.3855 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=32.4967 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=32.7751 μM	SANGER
MFH-ino	Growth Inhibition Assay			IC50=34.3224 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=34.6748 μM	SANGER
HUTU-80	Growth Inhibition Assay			IC50=35.3667 μM	SANGER
EB2	Growth Inhibition Assay			IC50=36.6189 μM	SANGER
L-540	Growth Inhibition Assay			IC50=37.2308 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=38.8846 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=39.9651 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=42.415 μM	SANGER
BC-3	Growth Inhibition Assay			IC50=45.4896 μM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=45.5474 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=45.666 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=46.018 μM	SANGER
SKBR3	Cytotoxicity assay			Cytotoxicity against human SKBR3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.002 μM.	21080629
SKOV3	Cytotoxicity assay			Cytotoxicity against human SKOV3 cells overexpressing HER2 by resazurin dye reduction assay, IC50 = 0.003 μM.	21080629
CAL27	Cytotoxicity assay			Cytotoxicity against human CAL27 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.007 μM.	21080629
4T1	Cytotoxicity assay			Cytotoxicity against mouse triple negative 4T1 cells, IC50 = 0.01037 μM.	24890652
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, IC50 = 0.011 μM.	25151582
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.017 μM.	19028425
MDA-MB-231	Cytotoxicity assay			Cytotoxicity against human triple negative MDA-MB-231 cells, IC50 = 0.02 μM.	24890652
BT474	Antiproliferative assay			Antiproliferative activity against human BT474 cells overexpressing ErB2, IC50 = 0.025 μM.	18653333
BT474	Antiproliferative assay		72 hrs	Antiproliferative activity against human BT474 cells after 72 hrs by methylene blue staining-based method, IC50 = 0.025 μM.	21887403
HEK293	Function assay			Inhibition of recombinant human C-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.02706 μM.	28711703
HEK293	Function assay			Inhibition of recombinant human N-terminal His-tagged EGFR (1 to 645 residues) expressed in HEK293 cells by ELISA, IC50 = 0.0271 μM.	29421573
HepG2	Function assay			Inhibition of EGFR in human HepG2 cells, IC50 = 0.0271 μM.	30096580
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells after 72 hrs by SRB assay, IC50 = 0.029 μM.	19888761
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells overexpressing HER-2 gene after 72 hrs by SRB assay, IC50 = 0.029 μM.	22372864
MDA-MB-435	Cytotoxicity assay			Cytotoxicity against human MDA-MB-435 cells, IC50 = 0.0297 μM.	24890652
SKBR3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKBR3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0301 μM.	25305330
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells expressing Her2 assessed as reduction in cell viability after 72 hrs by cell titer-glo luminescence assay, IC50 = 0.031 μM.	27288180
CAL27	Function assay		16 hrs	Inhibition of EGF-induced EGFR phosphorylation in human CAL27 cells overexpressing EGFR after 16 hrs by Western blot, IC50 = 0.032 μM.	21080629
NCI-N87	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-N87 cells expressing HER-2 after 72 hrs by SRB assay, IC50 = 0.036 μM.	22372864
insect cells	Function assay		5 mins	Inhibition of recombinant human EGFR L858R mutant expressed in baculovirus infected insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.03755 μM.	30096580
SK-BR-3	Antiproliferative assay			Antiproliferative activity against human SK-BR-3 cells after hrs by ATP content assay, IC50 = 0.04 μM.	20143778
MDA-MB-175	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-175 cells expressing Src, Ret and low HER-2 after 72 hrs by SRB assay, IC50 = 0.0444 μM.	22372864
A431	Function assay			Inhibition of EGFR intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.052 μM.	20346655
SK-BR-3	Antiproliferative assay		48 hrs	Antiproliferative activity against human SK-BR-3 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.06 μM.	27769671
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.0639 μM.	25305330
MCF7	Cytotoxicity assay			Cytotoxicity against human ER-positive MCF7 cells, IC50 = 0.0649 μM.	24890652
MDA-MB-468	Cytotoxicity assay			Cytotoxicity against human triple negative MDA-MB-468 cells, IC50 = 0.0832 μM.	24890652
NCI-N87	Antiproliferative assay		3 days	Antiproliferative activity against human NCI-N87 cells after 3 days by methylene blue staining, IC50 = 0.09 μM.	22101132
N87	Function assay			Inhibition of ErbB2 intracellular phosphorylation in human N87 cells by ELISA, IC50 = 0.1 μM.	20346655
BT474	Antiproliferative assay		3 days	Antiproliferative activity against human BT474 cells after 3 days by methylene blue staining, IC50 = 0.1 μM.	22101132
Calu3	Antiproliferative assay		72 hrs	Antiproliferative activity against human Calu3 cells after 72 hrs by MTT assay, IC50 = 0.1 μM.	28092860
BT474	Cytotoxicity assay		48 hrs	Cytotoxicity against human BT474 cells expressing HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.1 μM.	27769671
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells after 72 hrs by SRB assay, IC50 = 0.104 μM.	19888761
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells overexpressing HER-1 gene after 72 hrs by SRB assay, IC50 = 0.104 μM.	22372864
HeLa	Antiproliferative assay		12 hrs	Antiproliferative activity against human HeLa cells after 12 hrs by MTT assay, IC50 = 0.12 μM.	26652482
MIAPaCa	Function assay			Inhibition of ERBb2 phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.14 μM.	20817523
A431	Antiproliferative assay		48 hrs	Antiproliferative activity against human A431 cells expressing EGFR/HER2 assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.15 μM.	27769671
MDA-MB-453	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-453 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.19 μM.	25305330
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.2 μM.	29089259
B16F10	Antiproliferative assay		12 hrs	Antiproliferative activity against mouse B16F10 cells after 12 hrs by MTT assay, IC50 = 0.21 μM.	26652482
Sf21	Function assay		5 mins	Inhibition of N-terminal GST-tagged recombinant human EGFR T790M mutant expressed in baculovirus infected Sf21 insect cells preincubated for 5 mins followed by ATP addition and measured after 30 mins by HTRF assay, IC50 = 0.22489 μM.	30096580
Calu3	Cytotoxicity assay		72 hrs	Cytotoxicity against human Calu3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.23 μM.	25305330
DIFI	Cytotoxicity assay		4 days	Cytotoxicity against human DIFI cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.235 μM.	22169601
HepG2	Antiproliferative assay		12 hrs	Antiproliferative activity against human HepG2 cells after 12 hrs by MTT assay, IC50 = 0.27 μM.	26652482
EOL-1	Cytotoxicity assay		72 hrs	Cytotoxicity against human EOL-1 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 0.41 μM.	29089259
MIAPaCa	Function assay			Inhibition of EGFR phosphorylation in human MIAPaCa cells by ELISA, IC50 = 0.433 μM.	20817523
MCF7	Antiproliferative assay		12 hrs	Antiproliferative activity against human MCF7 cells after 12 hrs by MTT assay, IC50 = 0.47 μM.	26652482
SKBR3	Antiproliferative assay		48 hrs	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay, IC50 = 0.49 μM.	27187856
A549	Cytotoxicity assay		48 hrs	Cytotoxicity against human A549 cells expressing EGFR and KRAS mutant assessed as reduction in cell viability measured after 48 hrs by MTT assay, IC50 = 0.51 μM.	27769671
CAL27	Cytotoxicity assay		4 days	Cytotoxicity against human CAL27 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 0.53 μM.	22169601
MDA-MB-453	Cytotoxicity assay		72 hrs	Cytotoxicity against PTEN-deficient human MDA-MB-453 cells expressing HER-2, and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 0.555 μM.	22372864
SKOV3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKOV3 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.59 μM.	25305330
HCC827	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 del mutant after 72 hrs by MTT assay, IC50 = 0.6 μM.	29421573
A431NS	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431NS cells after 72 hrs by MTT assay, IC50 = 0.6 μM.	28092860
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 0.6431 μM.	25305330
BT474	Cytotoxicity assay		72 hrs	Cytotoxicity against human BT474 cells expressing HER2 after 72 hrs by Cell Titer Glo assay, GI50 = 0.93 μM.	26475520
A431	Cytotoxicity assay			Cytotoxicity against human A431 cells overexpressing EGFR by resazurin dye reduction assay, IC50 = 0.97 μM.	21080629
MDA-MB-361	Cytotoxicity assay		72 hrs	Cytotoxicity against ER activated human MDA-MB-361 cells expressing Her-2, Src and PIK3CA mutant after 72 hrs by SRB assay, IC50 = 1.029 μM.	22372864
GXF251L	Cytotoxicity assay		4 days	Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 1.48 μM.	22169601
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.6 μM.	22595177
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells overexpressing EGFR after 72 hrs by MTT assay, IC50 = 2.62 μM.	22182581
LXFA 629L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFA 629L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.87 μM.	22169601
DU145	Cytotoxicity assay		4 days	Cytotoxicity against human DU145 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 2.99 μM.	22169601
SKOV3	Cytotoxicity assay		72 hrs	Cytotoxicity against human SKOV3 cells overexpressing ErbB2 after 72 hrs by MTT assay, IC50 = 2.99 μM.	22182581
NCI-H1781	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1781 cells expressing HER-2 G776insV_G/C after 72 hrs by SRB assay, IC50 = 3.047 μM.	22372864
OVXF 899L	Cytotoxicity assay		4 days	Cytotoxicity against human OVXF 899L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.35 μM.	22169601
LXFL 529L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFL 529L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.51 μM.	22169601
LNCAP	Cytotoxicity assay		4 days	Cytotoxicity against human LNCAP cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 3.68 μM.	22169601
Bel7402	Antiproliferative assay		72 hrs	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay, IC50 = 3.7 μM.	28092860
LXFA 526L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFA 526L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.21 μM.	22169601
NIH/3T3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse NIH/3T3 cells after 72 hrs by MTT assay, IC50 = 4.3 μM.	22595177
SK-BR-3	Antiproliferative assay			Antiproliferative activity against ErbB2 overexpressing human SK-BR-3 cells by MTT assay, IC50 = 4.35 μM.	21570843
UXF 1138L	Cytotoxicity assay		4 days	Cytotoxicity against human UXF 1138L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.4 μM.	22169601
SK-BR-3	Antiproliferative assay		72 hrs	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay, IC50 = 4.4 μM.	28092860
PC3M	Cytotoxicity assay		4 days	Cytotoxicity against human PC3M cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.55 μM.	22169601
COLO205	Antiproliferative assay		72 hrs	Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay, IC50 = 4.6 μM.	28092860
HT-29	Cytotoxicity assay		4 days	Cytotoxicity against human HT-29 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.62 μM.	22169601
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM.	29421573
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 4.8 μM.	28711703
A431	Cytotoxicity assay		72 hrs	Cytotoxicity against human A431 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 4.8 μM.	28238614
MCF7	Cytotoxicity assay		4 days	Cytotoxicity against human MCF7 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.83 μM.	22169601
MEXF 1341L	Cytotoxicity assay		4 days	Cytotoxicity against human MEXF 1341L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 4.85 μM.	22169601
MCF7	Cytotoxicity assay		24 hrs	Cytotoxicity against human MCF7 cells after 24 hrs by SRB assay, IC50 = 5.02 μM.	30096580
SKBR3	Antiproliferative assay		72 hrs	Antiproliferative activity against human estrogen receptor and progesterone receptor deficient SKBR3 cells expressing HER2 after 72 hrs by MTT assay, IC50 = 5.05 μM.	23927972
SKHEP1	Antiproliferative assay		hrs	Antiproliferative activity against human SKHEP1 cells after hrs by ATP content assay, IC50 = 5.3 μM.	20143778
RKO	Cytotoxicity assay		4 days	Cytotoxicity against human RKO cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.35 μM.	22169601
MDA-MB-231	Antiproliferative assay		hrs	Antiproliferative activity against human MDA-MB-231 cells after hrs by ATP content assay, IC50 = 5.4 μM.	20143778
Hep3B2	Antiproliferative assay		hrs	Antiproliferative activity against human Hep3B2 cells after hrs by ATP content assay, IC50 = 5.49 μM.	20143778
K562	Cytotoxicity assay		72 hrs	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 5.7 μM.	29089259
LXFA 289L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFA 289L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.79 μM.	22169601
MAXF 401NL	Cytotoxicity assay		4 days	Cytotoxicity against human MAXF 401NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 5.8 μM.	22169601
HeLa	Cytotoxicity assay			Cytotoxicity against human HeLa cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 5.9 μM.	21080629
HCT116	Cytotoxicity assay		24 hrs	Cytotoxicity against human HCT116 cells after 24 hrs by SRB assay, IC50 = 5.92 μM.	30096580
22Rv1	Cytotoxicity assay		4 days	Cytotoxicity against human 22Rv1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.06 μM.	22169601
PAXF 546L	Cytotoxicity assay		4 days	Cytotoxicity against human PAXF 546L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.12 μM.	22169601
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.2 μM.	28092860
HepG2	Antiproliferative assay			Antiproliferative activity against human HepG2 cells after hrs by ATP content assay, IC50 = 6.27 μM.	20143778
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells assessed as reduction in cell viability, TC50 = 6.27 μM.	29049963
HepG2	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, TC50 = 6.3 μM.	30344906
NCI-H522	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H522 cells after 72 hrs by MTT assay, IC50 = 6.4 μM.	28092860
MCF7	Antiproliferative assay		hrs	Antiproliferative activity against human MCF7 cells after hrs by ATP content assay, IC50 = 6.6 μM.	20143778
A549	Antiproliferative assay		48 hrs	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 6.74 μM.	27187856
MCF7	Antiproliferative assay		72 hrs	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 6.8 μM.	29684708
PXF 1118L	Cytotoxicity assay		4 days	Cytotoxicity against human PXF 1118L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 6.86 μM.	22169601
LIXF 575L	Cytotoxicity assay		4 days	Cytotoxicity against human LIXF 575L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.18 μM.	22169601
RXF 1781L	Cytotoxicity assay		4 days	Cytotoxicity against human RXF 1781L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.67 μM.	22169601
MDA231	Cytotoxicity assay		4 days	Cytotoxicity against human MDA231 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.7 μM.	22169601
LXFL 1121L	Cytotoxicity assay		4 days	Cytotoxicity against human LXFL 1121L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.73 μM.	22169601
RXF 393NL	Cytotoxicity assay		4 days	Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 7.77 μM.	22169601
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 8.1 μM.	29089259
PANC1	Cytotoxicity assay		4 days	Cytotoxicity against human PANC1 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.12 μM.	22169601
CXF 269L	Cytotoxicity assay		4 days	Cytotoxicity against human CXF 269L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 8.36 μM.	22169601
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 8.4 μM.	28092860
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by sulforhodamine B assay, IC50 = 8.468 μM.	25305330
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells overexpressing HDAC by resazurin dye reduction assay, IC50 = 8.5 μM.	21080629
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay, IC50 = 9.08 μM.	28711703
NCI-H1975	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 9.08 μM.	28238614
RXF 486L	Cytotoxicity assay		4 days	Cytotoxicity against human RXF 486L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.1 μM.	22169601
Saos2	Cytotoxicity assay		4 days	Cytotoxicity against human Saos2 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.38 μM.	22169601
PXF 1752L	Cytotoxicity assay		4 days	Cytotoxicity against human PXF 1752L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.46 μM.	22169601
PXF 698L	Cytotoxicity assay		4 days	Cytotoxicity against human PXF 698L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.49 μM.	22169601
BXF T24	Cytotoxicity assay		4 days	Cytotoxicity against human BXF T24 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 9.65 μM.	22169601
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 10.12 μM.	29684708
MEXF 462NL	Cytotoxicity assay		4 days	Cytotoxicity against human MEXF 462NL cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.13 μM.	22169601
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by MTT assay, IC50 = 10.4 μM.	29684708
TE671	Cytotoxicity assay		4 days	Cytotoxicity against human TE671 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 10.95 μM.	22169601
RAW264.7	Antileishmanial assay		96 hrs	Antileishmanial activity against luciferase-expressing Leishmania major amastigotes infected in mouse RAW264.7 cells after 96 hrs by luminescence assay, EC50 = 11 μM.	28337329
PAXF 1657L	Cytotoxicity assay		4 days	Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.11 μM.	22169601
MEXF 276L	Cytotoxicity assay		4 days	Cytotoxicity against human MEXF 276L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.37 μM.	22169601
MKN45	Cytotoxicity assay		4 days	Cytotoxicity against human MKN45 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.48 μM.	22169601
BXF 1352L	Cytotoxicity assay		4 days	Cytotoxicity against human BXF 1352L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.53 μM.	22169601
HepG2	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay, IC50 = 11.71 μM.	30096580
BXF 1218L	Cytotoxicity assay		4 days	Cytotoxicity against human BXF 1218L cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 11.77 μM.	22169601
Caco	Cytotoxicity assay		24 hrs	Cytotoxicity against human Caco cells after 24 hrs by SRB assay, IC50 = 12.11 μM.	30096580
SW480	Antiproliferative assay		72 hrs	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM.	29421573
SW480	Antiproliferative assay		72 hrs	Antiproliferative activity against human SW480 cells harboring wild type EGFR after 72 hrs by MTT assay, IC50 = 12.58 μM.	28711703
SW480	Cytotoxicity assay		72 hrs	Cytotoxicity against human SW480 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 12.58 μM.	28238614
NCI-H1975	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay, IC50 = 12.68 μM.	29421573
3T3	Antitrypanosomal assay		48 hrs	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen amastigotes infected in rat 3T3 cells after 48 hrs by chlorophenol red-beta-D-galactopyranoside based assay, EC50 = 13 μM.	28337329
HCT116	Cytotoxicity assay		4 days	Cytotoxicity against human HCT116 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.14 μM.	22169601
OVCAR3	Cytotoxicity assay		4 days	Cytotoxicity against human OVCAR3 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.44 μM.	22169601
H460	Cytotoxicity assay		4 days	Cytotoxicity against human H460 cells after 4 days by propidium iodide staining-based fluorometric analysis, IC50 = 13.46 μM.	22169601
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM.	29421573
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells harboring wild type EGFR/K-Ras mutant after 72 hrs by MTT assay, IC50 = 14.9 μM.	28711703
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IG50 = 14.9 μM.	28238614
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells expressing pcDNA3 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.71 μM.	24355130
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells expressing HER2 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 15.79 μM.	24355130
MCF7	Cytotoxicity assay		48 hrs	Cytotoxicity against human MCF7 cells expressing HER2delta16 assessed as reduction of cell viability after 48 hrs CellTiter-Glo assay, IC50 = 19.22 μM.	24355130
MDA-MB-468	Antiproliferative assay		72 hrs	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay, IC50 = 20 μM.	28092860
HCC827	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCC827 cells assessed as growth inhibition after 72 hrs by calcein-AM dye based fluorescence assay, GI50 = 22.3 μM.	29089259
MDA-MB-468	Antiproliferative assay			Antiproliferative activity against EGFR overexpressing human MDA-MB-468 cells by MTT assay, IC50 = 23.46 μM.	21570843
HCT116	Antiproliferative assay			Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 42.36 μM.	21570843
NCI-N87	Antitumor assay			Antitumor activity against human NCI-N87 cells xenografted in athymic mouse assessed as tumor growth inhibition at 20 mg/kg, po QD for 14 days measured after 19 days	22101132
A431	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
A431	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER1 (unknown origin) expressed in human A431 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
BT474	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in ERK1/2 phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
BT474	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER2 (unknown origin) expressed in human BT474 cells assessed as reduction in AKT phosphorylation at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
A431	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER1 phosphorylation (unknown origin) expressed in human A431 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
BT474	Function assay	0.001 to 10 uM	2 hrs	Inhibition of HER2 phosphorylation (unknown origin) expressed in human BT474 cells at 0.001 to 10 uM incubated for 2 hrs by Western blot method	25305330
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
NCI-H522	Antitumor assay			Antitumor activity against human NCI-H522 cells xenografted in Balb/c nude mouse assessed as tumor growth inhibition at 100 mg/kg, ig administered once daily for 28 days relative to control	28092860
MCF7	Function assay	10 uM	2 hrs	Inhibition of HER2 delta16 mutant autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2delta16 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing HER2 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of EGFR autophosphorylation at Y1068 in human MCF7 cells expressing pcDNA3 at 10 uM after 2 hrs by Western blotting	24355130
MCF7	Function assay	10 uM	2 hrs	Inhibition of HER2 autophosphorylation at Y1248 in human MCF7 cells at 10 uM after 2 hrs by Western blotting	24355130
A549	Function assay	50 uM	2 hrs	Inhibition of EGFR phosphorylation at Y1068 in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method	28238614
A549	Function assay	50 uM	2 hrs	Inhibition of EGFR phosphorylation at Tyr residue in human A549 cells at 50 uM preincubated for 2 hrs followed by EGF induction measured after 10 mins by Western blot method	28238614
LLC	Antitumor assay			Antitumor activity against mouse LLC cells implanted in in C57BL/6 mouse assessed as tumor growth inhibition at 100 mg/kg, po qd for 14 days	27187856
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità

Peso molecolare	581.06	Formula	C₂₉H₂₆ClFN₄O₄S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	231277-92-2	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	GSK572016, GW2016			Smiles	CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl

Solubilità

In vitro
Lotto:

DMSO : 100 mg/mL (172.09 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	ErbB2 (Cell-free assay) 9.2 nM EGFR (Cell-free assay) 10.8 nM ErbB4 (Cell-free assay) 367 nM
In vitro	Lapatinib inibisce debolmente l'attività di ErbB4 con un IC50 di 367 nM e mostra una selettività >300 volte superiore per EGFR ed ErbB2 rispetto ad altre chinasi come c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2 e VEGFR2. Questo composto inibisce significativamente l'autofosforilazione dei recettori EGFR ed ErbB2 in modo dose-dipendente con IC50 di 170 nM e 80 nM, rispettivamente, nelle cellule HN5; così come 210 nM e 60 nM, rispettivamente, nelle cellule BT474. A differenza di OSI-774 e Iressa (ZD1839) che inibiscono preferenzialmente la crescita delle cellule sovraesprimenti EGFR, inibisce la crescita sia delle cellule sovraesprimenti EGFR che delle cellule sovraesprimenti ErbB2. Questa sostanza chimica mostra una maggiore attività inibitoria contro le cellule sovraesprimenti EGFR o ErbB2 con un IC50 di 0,09-0,21 μM, rispetto alle cellule che esprimono bassi livelli di EGFR o ErbB2 con un IC50 di 3-12 μM, ed esibisce una selettività di circa 100 volte rispetto alle normali cellule fibroblastiche. Inibisce potentemente la crescita delle cellule HN5 e A-431 sovraesprimenti EGFR, così come delle cellule BT474 e N87 sovraesprimenti ErbB2, e induce significativamente l'arresto in fase G1 delle cellule HN5 e l'apoptosi delle cellule BT474, che sono associate all'inibizione della fosforilazione di AKT.
Saggio chinasico	Saggi chinasici in vitro
Saggio chinasico	I valori di IC50 per l'inibizione dell'attività enzimatica sono generati misurando l'inibizione della fosforilazione di un substrato peptidico. I domini chinasici intracellulari di EGFR ed ErbB2 sono purificati da un sistema di espressione a baculovirus. Le reazioni di EGFR ed ErbB2 vengono eseguite in piastre a 96 pozzetti con fondo arrotondato in polistirene in un volume finale di 45 μL. Le miscele di reazione contengono 50 mM di acido 4-morfolinopropansolfonico (pH 7,5), 2 mM di MnCl₂, 10 μM di ATP, 1 μCi di [γ³³P] ATP/reazione, 50 μM di Peptide A [Biotina-(acido amino esanoico)-EEEEYFELVAKKK-CONH2], 1 mM di ditiotreitolo e 1 μL di DMSO contenente diluizioni seriali di questo composto a partire da 10 μM. La reazione è iniziata aggiungendo il dominio intracellulare purificato del recettore di tipo 1 indicato. La quantità di enzima aggiunta è di 1 pmol/reazione (20 nM). Le reazioni sono terminate dopo 10 minuti a 23°C aggiungendo 45 μL di acido fosforico allo 0,5% in acqua. La miscela di reazione terminata (75 μL) viene trasferita su piastre filtranti di fosfocellulosa. Le piastre vengono filtrate e lavate tre volte con 200 μL di acido fosforico allo 0,5%. Un cocktail di scintillazione (50 μL) viene aggiunto a ciascun pozzetto e il saggio viene quantificato mediante conteggio in un Packard Topcount. I valori di IC50 vengono generati da curve dose-risposta a 10 punti.
In vivo	La somministrazione orale di Lapatinib (~100 mg/kg) due volte al giorno inibisce significativamente la crescita di xenotrapianti BT474 e HN5 in modo dose-dipendente.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/12467226/

Applicazioni

Metodi	Biomarcatori	PMID
Western blot	ERBB2 / pERBB2 / p53 / Mdm2 / MdmX / pERK / Hsp70 pEGFR / EGFR / pAkt / Akt / pmTOR / mTOR / PARP / c-PARP p-HER2 / HER2 / p-HER3 / HER3 / p-S6 / S6 / p-4EBP1	29799521
Immunofluorescence	LC3 Vimentin / E-cadherin	26637440
Growth inhibition assay	Cell viability (OE19) Cell viability (A431 cells)	25350844

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT00455039	Withdrawn	Breast Cancer	University of New Mexico	July 31 2023	Phase 1\|Phase 2
NCT04608409	Active not recruiting	Ovarian Cancer	Frederick R. Ueland M.D.\|National Cancer Institute (NCI)\|University of Kentucky	March 17 2021	Phase 1
NCT03075995	Unknown status	Breast Cancer	Sun Yat-sen University	April 12 2017	Not Applicable
NCT02338245	Completed	Metastatic Breast Cancer	ASLAN Pharmaceuticals	December 29 2014	Phase 2
NCT02294786	Terminated	Cancer	Novartis Pharmaceuticals\|Novartis	December 17 2014	Phase 2
NCT02158507	Active not recruiting	Metastatic Triple Negative Breast Cancer	University of Alabama at Birmingham\|Breast Cancer Research Foundation of Alabama\|GlaxoSmithKline\|AbbVie	September 2014	Not Applicable

Supporto tecnico

Istruzioni per la manipolazione

Tel: +1-832-582-8158 Ext:3

Per qualsiasi altra domanda, si prega di lasciare un messaggio.

Domande Frequenti

Domanda 1:
If I want to use this compound via injection in tumor-bearing mice, how could I prepare the solution?

Risposta:
For I.P. administration, the compound solution should be clear solution. It can be dissolved in 2% DMSO/30% PEG 300/5% Tween 80/ddH2O at 10 mg/ml for clear solution.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):