Home Protein Tyrosine Kinase IGF-1R inhibitor Linsitinib (OSI-906)

solo per uso di ricerca

Linsitinib (OSI-906) IGF-1R/Insulin Receptor inhibitor

N. Cat.: S1091

Linsitinib (OSI-906) is a selective inhibitor of IGF-1R with IC50 of 35 nM in cell-free assays. It is modestly potent to InsR with IC50 of 75 nM, and shows no activity towards Abl, ALK, BTK, EGFR, FGFR1/2, PKA etc. Phase 3.
Linsitinib (OSI-906) IGF-1R inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 421.49

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.99%
99.99

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività PMID
A4-Fuk Growth Inhibition Assay IC50=0.02806 μM SANGER
KS-1 Growth Inhibition Assay IC50=0.03835 μM SANGER
TE-11 Growth Inhibition Assay IC50=0.07822 μM SANGER
EW-1 Growth Inhibition Assay IC50=0.08585 μM SANGER
HMV-II Growth Inhibition Assay IC50=0.08846 μM SANGER
COLO-205 Growth Inhibition Assay IC50=0.10454 μM SANGER
ES1 Growth Inhibition Assay IC50=0.10696 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.13672 μM SANGER
ML-2 Growth Inhibition Assay IC50=0.15896 μM SANGER
Saos-2 Growth Inhibition Assay IC50=0.16526 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=0.18135 μM SANGER
G-401 Growth Inhibition Assay IC50=0.1823 μM SANGER
EW-16 Growth Inhibition Assay IC50=0.18777 μM SANGER
EW-7 Growth Inhibition Assay IC50=0.18881 μM SANGER
NCI-H727 Growth Inhibition Assay IC50=0.19794 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=0.20955 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=0.21384 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=0.23299 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=0.23698 μM SANGER
HT-29 Growth Inhibition Assay IC50=0.24248 μM SANGER
LB771-HNC Growth Inhibition Assay IC50=0.25915 μM SANGER
HT-144 Growth Inhibition Assay IC50=0.26191 μM SANGER
LAN-6 Growth Inhibition Assay IC50=0.26348 μM SANGER
EW-18 Growth Inhibition Assay IC50=0.27001 μM SANGER
LS-1034 Growth Inhibition Assay IC50=0.27132 μM SANGER
EW-11 Growth Inhibition Assay IC50=0.28432 μM SANGER
SNU-C1 Growth Inhibition Assay IC50=0.29313 μM SANGER
RS4-11 Growth Inhibition Assay IC50=0.33758 μM SANGER
ES4 Growth Inhibition Assay IC50=0.41038 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=0.41368 μM SANGER
NB10 Growth Inhibition Assay IC50=0.45437 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=0.46758 μM SANGER
A375 Growth Inhibition Assay IC50=0.47617 μM SANGER
SJRH30 Growth Inhibition Assay IC50=0.50822 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.52267 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=0.53557 μM SANGER
DOK Growth Inhibition Assay IC50=0.556 μM SANGER
NB69 Growth Inhibition Assay IC50=0.58257 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=0.60236 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=0.65491 μM SANGER
NCI-H358 Growth Inhibition Assay IC50=0.67082 μM SANGER
RH-1 Growth Inhibition Assay IC50=0.74859 μM SANGER
NH-12 Growth Inhibition Assay IC50=0.76046 μM SANGER
TE-12 Growth Inhibition Assay IC50=0.76486 μM SANGER
COLO-668 Growth Inhibition Assay IC50=0.84666 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=0.86377 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.88263 μM SANGER
ABC-1 Growth Inhibition Assay IC50=0.90352 μM SANGER
ES6 Growth Inhibition Assay IC50=0.91066 μM SANGER
SNU-387 Growth Inhibition Assay IC50=0.99393 μM SANGER
CMK Growth Inhibition Assay IC50=0.99929 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=1.03653 μM SANGER
SIMA Growth Inhibition Assay IC50=1.06825 μM SANGER
ES3 Growth Inhibition Assay IC50=1.12297 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=1.15444 μM SANGER
MEL-JUSO Growth Inhibition Assay IC50=1.15759 μM SANGER
T84 Growth Inhibition Assay IC50=1.20914 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=1.23138 μM SANGER
RD Growth Inhibition Assay IC50=1.26455 μM SANGER
TE-8 Growth Inhibition Assay IC50=1.31462 μM SANGER
L-363 Growth Inhibition Assay IC50=1.34208 μM SANGER
EKVX Growth Inhibition Assay IC50=1.34568 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=1.48556 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=1.50193 μM SANGER
NCI-H1770 Growth Inhibition Assay IC50=1.51113 μM SANGER
HuH-7 Growth Inhibition Assay IC50=1.60098 μM SANGER
HL-60 Growth Inhibition Assay IC50=1.66928 μM SANGER
TE-1 Growth Inhibition Assay IC50=1.70945 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=1.73887 μM SANGER
LB647-SCLC Growth Inhibition Assay IC50=1.76583 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=1.77716 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=1.91298 μM SANGER
MC-IXC Growth Inhibition Assay IC50=1.9898 μM SANGER
LS-513 Growth Inhibition Assay IC50=2.05305 μM SANGER
EW-3 Growth Inhibition Assay IC50=2.09844 μM SANGER
OPM-2 Growth Inhibition Assay IC50=2.102 μM SANGER
LP-1 Growth Inhibition Assay IC50=2.25807 μM SANGER
LU-134-A Growth Inhibition Assay IC50=2.277 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=2.29014 μM SANGER
HCC1143 Growth Inhibition Assay IC50=2.45368 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=2.6021 μM SANGER
TE-10 Growth Inhibition Assay IC50=2.70838 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=2.75227 μM SANGER
CHP-126 Growth Inhibition Assay IC50=2.76317 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=2.92024 μM SANGER
GB-1 Growth Inhibition Assay IC50=2.93404 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=2.95281 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=2.96896 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=3.00565 μM SANGER
NCI-H526 Growth Inhibition Assay IC50=3.04085 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=3.04992 μM SANGER
SNU-423 Growth Inhibition Assay IC50=3.20313 μM SANGER
A427 Growth Inhibition Assay IC50=3.25699 μM SANGER
CAL-12T Growth Inhibition Assay IC50=3.40713 μM SANGER
LU-99A Growth Inhibition Assay IC50=3.47105 μM SANGER
MS-1 Growth Inhibition Assay IC50=3.53429 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=3.76295 μM SANGER
SW837 Growth Inhibition Assay IC50=3.76333 μM SANGER
ES8 Growth Inhibition Assay IC50=3.83877 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=3.92086 μM SANGER
TGW Growth Inhibition Assay IC50=4.01311 μM SANGER
GP5d Growth Inhibition Assay IC50=4.05362 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=4.15213 μM SANGER
NB13 Growth Inhibition Assay IC50=4.26887 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=4.28615 μM SANGER
NCI-H1648 Growth Inhibition Assay IC50=4.29819 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=4.32195 μM SANGER
LS-411N Growth Inhibition Assay IC50=4.44885 μM SANGER
NCI-H1092 Growth Inhibition Assay IC50=4.45687 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=4.6984 μM SANGER
DK-MG Growth Inhibition Assay IC50=4.80933 μM SANGER
OVCAR-5 Growth Inhibition Assay IC50=4.81226 μM SANGER
CAL-39 Growth Inhibition Assay IC50=4.8767 μM SANGER
TE-441-T Growth Inhibition Assay IC50=4.90537 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=4.95253 μM SANGER
MCF7 Growth Inhibition Assay IC50=5.14517 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=5.25707 μM SANGER
PSN1 Growth Inhibition Assay IC50=5.27235 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=5.30044 μM SANGER
CPC-N Growth Inhibition Assay IC50=5.39419 μM SANGER
DoTc2-4510 Growth Inhibition Assay IC50=5.45371 μM SANGER
LB1047-RCC Growth Inhibition Assay IC50=5.55933 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=5.59907 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=5.70227 μM SANGER
SW1710 Growth Inhibition Assay IC50=5.74751 μM SANGER
YAPC Growth Inhibition Assay IC50=5.76201 μM SANGER
22RV1 Growth Inhibition Assay IC50=5.80019 μM SANGER
COLO-679 Growth Inhibition Assay IC50=5.88948 μM SANGER
TCCSUP Growth Inhibition Assay IC50=5.93259 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=5.9397 μM SANGER
TE-15 Growth Inhibition Assay IC50=6.06605 μM SANGER
SCLC-21H Growth Inhibition Assay IC50=6.10843 μM SANGER
EoL-1-cell Growth Inhibition Assay IC50=6.16563 μM SANGER
NKM-1 Growth Inhibition Assay IC50=6.1671 μM SANGER
NCI-H1304 Growth Inhibition Assay IC50=6.27428 μM SANGER
NB6 Growth Inhibition Assay IC50=6.29622 μM SANGER
NALM-6 Growth Inhibition Assay IC50=6.3323 μM SANGER
NCI-H522 Growth Inhibition Assay IC50=6.33306 μM SANGER
MV-4-11 Growth Inhibition Assay IC50=6.37079 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=6.38667 μM SANGER
NCI-H1417 Growth Inhibition Assay IC50=6.40847 μM SANGER
HT-1197 Growth Inhibition Assay IC50=6.57122 μM SANGER
P30-OHK Growth Inhibition Assay IC50=6.6277 μM SANGER
ALL-PO Growth Inhibition Assay IC50=6.71916 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=6.75405 μM SANGER
HCC2157 Growth Inhibition Assay IC50=6.77475 μM SANGER
NCI-H838 Growth Inhibition Assay IC50=6.9649 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=6.9709 μM SANGER
SW954 Growth Inhibition Assay IC50=7.20068 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=7.34065 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=7.48373 μM SANGER
KARPAS-45 Growth Inhibition Assay IC50=7.65929 μM SANGER
CAL-54 Growth Inhibition Assay IC50=7.82977 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=7.88941 μM SANGER
NCI-H187 Growth Inhibition Assay IC50=7.95947 μM SANGER
RT-112 Growth Inhibition Assay IC50=8.09677 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=8.09795 μM SANGER
SNU-449 Growth Inhibition Assay IC50=8.28272 μM SANGER
HCC1187 Growth Inhibition Assay IC50=8.29391 μM SANGER
NCI-H2030 Growth Inhibition Assay IC50=8.37714 μM SANGER
HuO-3N1 Growth Inhibition Assay IC50=8.37844 μM SANGER
COLO-792 Growth Inhibition Assay IC50=8.41527 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=8.85508 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=9.0425 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=9.09751 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=9.10469 μM SANGER
ETK-1 Growth Inhibition Assay IC50=9.29974 μM SANGER
NCI-H1993 Growth Inhibition Assay IC50=9.44261 μM SANGER
no-11 Growth Inhibition Assay IC50=9.4712 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=9.51583 μM SANGER
NCCIT Growth Inhibition Assay IC50=9.53169 μM SANGER
SAS Growth Inhibition Assay IC50=10.248 μM SANGER
A673 Growth Inhibition Assay IC50=10.3704 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=10.3707 μM SANGER
NCI-H810 Growth Inhibition Assay IC50=10.3907 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=10.4564 μM SANGER
GR-ST Growth Inhibition Assay IC50=10.5024 μM SANGER
SUP-T1 Growth Inhibition Assay IC50=10.7317 μM SANGER
NB5 Growth Inhibition Assay IC50=10.9022 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=10.9571 μM SANGER
SK-CO-1 Growth Inhibition Assay IC50=10.9931 μM SANGER
Capan-2 Growth Inhibition Assay IC50=11.3198 μM SANGER
697 Growth Inhibition Assay IC50=11.6757 μM SANGER
REH Growth Inhibition Assay IC50=11.7451 μM SANGER
GI-1 Growth Inhibition Assay IC50=11.8615 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=12.0916 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=12.2478 μM SANGER
NCI-H1618 Growth Inhibition Assay IC50=12.3976 μM SANGER
NCI-H2081 Growth Inhibition Assay IC50=12.6141 μM SANGER
GCIY Growth Inhibition Assay IC50=12.7213 μM SANGER
NY Growth Inhibition Assay IC50=13.0643 μM SANGER
PANC-03-27 Growth Inhibition Assay IC50=13.0807 μM SANGER
BHY Growth Inhibition Assay IC50=13.2121 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=13.3763 μM SANGER
5637 Growth Inhibition Assay IC50=13.7759 μM SANGER
LC-1F Growth Inhibition Assay IC50=14.0356 μM SANGER
SNB75 Growth Inhibition Assay IC50=14.0383 μM SANGER
CHP-212 Growth Inhibition Assay IC50=14.0464 μM SANGER
HT-1376 Growth Inhibition Assay IC50=14.1126 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=14.1502 μM SANGER
CA46 Growth Inhibition Assay IC50=14.1827 μM SANGER
SCC-15 Growth Inhibition Assay IC50=14.5583 μM SANGER
ATN-1 Growth Inhibition Assay IC50=14.6627 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=14.8157 μM SANGER
NCI-H716 Growth Inhibition Assay IC50=14.8493 μM SANGER
SW620 Growth Inhibition Assay IC50=14.9014 μM SANGER
NCI-H226 Growth Inhibition Assay IC50=14.9085 μM SANGER
SW962 Growth Inhibition Assay IC50=14.9432 μM SANGER
KYSE-150 Growth Inhibition Assay IC50=14.955 μM SANGER
OCUB-M Growth Inhibition Assay IC50=14.9883 μM SANGER
ES7 Growth Inhibition Assay IC50=15.0984 μM SANGER
SW1463 Growth Inhibition Assay IC50=15.4223 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=15.5346 μM SANGER
MKN28 Growth Inhibition Assay IC50=15.5479 μM SANGER
SW13 Growth Inhibition Assay IC50=15.618 μM SANGER
A3-KAW Growth Inhibition Assay IC50=15.9697 μM SANGER
LU-65 Growth Inhibition Assay IC50=15.9768 μM SANGER
Calu-1 Growth Inhibition Assay IC50=16.0368 μM SANGER
ST486 Growth Inhibition Assay IC50=16.0431 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=16.1246 μM SANGER
EGI-1 Growth Inhibition Assay IC50=16.446 μM SANGER
SH-4 Growth Inhibition Assay IC50=16.4731 μM SANGER
MN-60 Growth Inhibition Assay IC50=17.2297 μM SANGER
MPP-89 Growth Inhibition Assay IC50=17.2459 μM SANGER
A2780 Growth Inhibition Assay IC50=17.4139 μM SANGER
Daoy Growth Inhibition Assay IC50=17.4695 μM SANGER
NCI-H2126 Growth Inhibition Assay IC50=17.4771 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=17.4917 μM SANGER
8-MG-BA Growth Inhibition Assay IC50=17.6648 μM SANGER
786-0 Growth Inhibition Assay IC50=17.8353 μM SANGER
AM-38 Growth Inhibition Assay IC50=17.9306 μM SANGER
COLO-824 Growth Inhibition Assay IC50=18.4436 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=18.5082 μM SANGER
CESS Growth Inhibition Assay IC50=18.7609 μM SANGER
BL-70 Growth Inhibition Assay IC50=18.8156 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=18.9179 μM SANGER
HT-3 Growth Inhibition Assay IC50=18.983 μM SANGER
BOKU Growth Inhibition Assay IC50=19.0381 μM SANGER
HPAF-II Growth Inhibition Assay IC50=19.3015 μM SANGER
KGN Growth Inhibition Assay IC50=19.4765 μM SANGER
MC-CAR Growth Inhibition Assay IC50=19.6313 μM SANGER
BHT-101 Growth Inhibition Assay IC50=19.777 μM SANGER
SW1783 Growth Inhibition Assay IC50=19.7806 μM SANGER
KP-N-YN Growth Inhibition Assay IC50=20.0262 μM SANGER
LU-165 Growth Inhibition Assay IC50=20.5571 μM SANGER
GOTO Growth Inhibition Assay IC50=20.6451 μM SANGER
EFM-19 Growth Inhibition Assay IC50=21.0716 μM SANGER
CTV-1 Growth Inhibition Assay IC50=21.1054 μM SANGER
HEL Growth Inhibition Assay IC50=21.4216 μM SANGER
SNU-C2B Growth Inhibition Assay IC50=21.426 μM SANGER
ECC4 Growth Inhibition Assay IC50=21.707 μM SANGER
NEC8 Growth Inhibition Assay IC50=21.8368 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=21.8921 μM SANGER
NCI-H524 Growth Inhibition Assay IC50=22.0808 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=22.1577 μM SANGER
SF126 Growth Inhibition Assay IC50=22.2469 μM SANGER
HOP-92 Growth Inhibition Assay IC50=22.3167 μM SANGER
CTB-1 Growth Inhibition Assay IC50=22.4677 μM SANGER
KYSE-270 Growth Inhibition Assay IC50=22.9357 μM SANGER
SK-MEL-24 Growth Inhibition Assay IC50=23.187 μM SANGER
Calu-3 Growth Inhibition Assay IC50=23.2128 μM SANGER
GAMG Growth Inhibition Assay IC50=23.2367 μM SANGER
SW1573 Growth Inhibition Assay IC50=23.7415 μM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=24.0194 μM SANGER
TK10 Growth Inhibition Assay IC50=24.5013 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=24.6064 μM SANGER
KALS-1 Growth Inhibition Assay IC50=24.7327 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=25.8032 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=26.1674 μM SANGER
OE19 Growth Inhibition Assay IC50=26.2153 μM SANGER
J82 Growth Inhibition Assay IC50=26.2471 μM SANGER
DU-4475 Growth Inhibition Assay IC50=26.3819 μM SANGER
DMS-53 Growth Inhibition Assay IC50=26.5138 μM SANGER
COLO-741 Growth Inhibition Assay IC50=26.8344 μM SANGER
SW48 Growth Inhibition Assay IC50=26.882 μM SANGER
IGR-1 Growth Inhibition Assay IC50=26.9334 μM SANGER
639-V Growth Inhibition Assay IC50=27.0245 μM SANGER
LK-2 Growth Inhibition Assay IC50=27.4141 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=27.9699 μM SANGER
NCI-H2228 Growth Inhibition Assay IC50=28.0905 μM SANGER
LS-123 Growth Inhibition Assay IC50=28.1262 μM SANGER
U031 Growth Inhibition Assay IC50=28.252 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=28.4721 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=28.7552 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=29.5208 μM SANGER
SW626 Growth Inhibition Assay IC50=29.756 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=29.815 μM SANGER
RXF393 Growth Inhibition Assay IC50=30.0952 μM SANGER
LC4-1 Growth Inhibition Assay IC50=30.3092 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=30.6624 μM SANGER
K5 Growth Inhibition Assay IC50=30.9702 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=30.9725 μM SANGER
BCPAP Growth Inhibition Assay IC50=31.8379 μM SANGER
BC-3 Growth Inhibition Assay IC50=32.1403 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=32.2358 μM SANGER
NCI-H2009 Growth Inhibition Assay IC50=32.4981 μM SANGER
HTC-C3 Growth Inhibition Assay IC50=33.7519 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=34.4407 μM SANGER
CCRF-CEM Growth Inhibition Assay IC50=34.5715 μM SANGER
AN3-CA Growth Inhibition Assay IC50=35.0568 μM SANGER
NCI-H1734 Growth Inhibition Assay IC50=35.2561 μM SANGER
Ca-Ski Growth Inhibition Assay IC50=35.4101 μM SANGER
U-266 Growth Inhibition Assay IC50=35.6114 μM SANGER
SBC-5 Growth Inhibition Assay IC50=35.7781 μM SANGER
GT3TKB Growth Inhibition Assay IC50=37.115 μM SANGER
MDA-MB-175-VII Growth Inhibition Assay IC50=37.2248 μM SANGER
PFSK-1 Growth Inhibition Assay IC50=37.2435 μM SANGER
IMR-5 Growth Inhibition Assay IC50=37.2487 μM SANGER
Daudi Growth Inhibition Assay IC50=37.3597 μM SANGER
A498 Growth Inhibition Assay IC50=37.7218 μM SANGER
SCC-4 Growth Inhibition Assay IC50=37.7843 μM SANGER
COLO-680N Growth Inhibition Assay IC50=38.2885 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=38.3215 μM SANGER
SR Growth Inhibition Assay IC50=38.5495 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=38.5637 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=38.7822 μM SANGER
BPH-1 Growth Inhibition Assay IC50=38.8329 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=39.5817 μM SANGER
LXF-289 Growth Inhibition Assay IC50=39.8084 μM SANGER
SW1088 Growth Inhibition Assay IC50=40.2107 μM SANGER
MOLT-4 Growth Inhibition Assay IC50=40.2901 μM SANGER
AsPC-1 Growth Inhibition Assay IC50=40.4583 μM SANGER
HOP-62 Growth Inhibition Assay IC50=40.6568 μM SANGER
A172 Growth Inhibition Assay IC50=40.8511 μM SANGER
SN12C Growth Inhibition Assay IC50=40.9385 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=40.9898 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=41.1593 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=41.8123 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=42.4697 μM SANGER
HSC-3 Growth Inhibition Assay IC50=42.6661 μM SANGER
PC-14 Growth Inhibition Assay IC50=43.1882 μM SANGER
COR-L105 Growth Inhibition Assay IC50=43.6502 μM SANGER
BE-13 Growth Inhibition Assay IC50=44.2371 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=44.2958 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=44.3599 μM SANGER
HCC1806 Growth Inhibition Assay IC50=44.5873 μM SANGER
COLO-800 Growth Inhibition Assay IC50=44.8453 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=45.1247 μM SANGER
8305C Growth Inhibition Assay IC50=45.309 μM SANGER
UACC-62 Growth Inhibition Assay IC50=46.2875 μM SANGER
COR-L23 Growth Inhibition Assay IC50=47.199 μM SANGER
EFE-184 Growth Inhibition Assay IC50=47.388 μM SANGER
DMS-114 Growth Inhibition Assay IC50=47.4149 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=48.5315 μM SANGER
SNG-M Growth Inhibition Assay IC50=49.434 μM SANGER
A2058 Growth Inhibition Assay IC50=49.4885 μM SANGER
HEK293 Function assay 60 mins Inhibition of full length IGF-1 receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.0028 μM. 26951753
Ba/F3 Function assay Inhibition of full length IGF-1 receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.0076 μM. 26951753
HEK293 Function assay 60 mins Inhibition of full length insulin receptor (unknown origin) autophosphorylation transfected in HEK293 cells pretreated for 60 mins followed by IGF-1 stimulation measured after 10 mins by quantitative Western blot analysis, IC50 = 0.016 μM. 26951753
A431 Function assay Inhibition of IGF1R intracellular phosphorylation in human A431 cells by ELISA, IC50 = 0.018 μM. 20346655
3T3 Function assay Inhibition of human IGF1R expressed in mouse 3T3 cells by ELISA based assay, IC50 = 0.024 μM. 21251824
NIH 3T3 Function assay 2 hrs Inhibition of full length human IGF-1R overexpressed in mouse NIH 3T3 cells assessed as IGF1-induced protein phosphorylation incubated for 2 hrs prior to IGF1 induction measured after 15 mins by ELISA, IC50 = 0.024 μM. 24900721
Ba/F3 Function assay Inhibition of full length insulin receptor (unknown origin) transfected in Ba/F3 cells assessed as cell proliferation, IC50 = 0.126 μM. 26951753
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary 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
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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 421.49 Formula

C26H23N5O

 Conservazione (Dalla data di ricezione)
N. CAS 867160-71-2 Scarica SDF Conservazione delle soluzioni stock

Sinonimi N/A Smiles CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 84 mg/mL (199.29 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:

Calcolatore di formulazione in vivo (Soluzione chiara)

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

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è 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, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (Mechanism of Action)

Targets/IC50/Ki
IGF-1R
(Cell-free assay)
35 nM
Insulin Receptor
(Cell-free assay)
75 nM
IRR
(Cell-free assay)
75 nM
In vitro
Linsitinib (OSI-906) inibisce l'autofosforilazione di IGF-1R e l'attivazione delle proteine di segnalazione a valle Akt, ERK1/2 e S6 chinasi con IC50 da 0,028 a 0,13 μM. Consente una conformazione intermedia della proteina bersaglio attraverso interazioni con l'elica C e mostra una favorevole stabilità metabolica nei microsomi epatici. Questo composto inibisce completamente la fosforilazione sia di IR che di IGF-1R a una concentrazione di 1 μM e inibisce la proliferazione di diverse linee cellulari tumorali, incluso il cancro al polmone non a piccole cellule e la linea cellulare tumorale del cancro colorettale (CRC) con EC50 da 0,021 a 0,810 μM.
Saggio chinasico
saggi biochimici di Protein Tyrosine Kinase
I saggi delle Protein Tyrosine Kinase vengono eseguiti internamente con metodi basati su ELISA (IGF-1R, IR, EGFR e KDR) o presso Upstate Inc. con un metodo radiometrico con ATP a una concentrazione di 100 µM. I saggi ELISA interni utilizzano poli(Glu:Tyr) come substrato legato alla superficie di piastre di saggio a 96 pozzetti e la fosforilazione viene rilevata utilizzando un anticorpo antifosfotirosina coniugato alla perossidasi di rafano. L'anticorpo legato viene quantificato utilizzando ABTS come substrato della perossidasi misurando l'assorbanza a 405/490 nm. Tutti i saggi utilizzano domini catalitici di chinasi ricombinanti purificati. Gli enzimi ricombinanti di IGF-1R o EGFR umani sono espressi come proteina di fusione glutatione S-transferasi NH2-terminale in cellule di insetto e sono purificati internamente. I valori di IC50 sono determinati dal grafico sigmoide dose-risposta della percentuale di inibizione rispetto al log10 della concentrazione del composto. Vengono eseguite un minimo di tre misurazioni, in duplicato, con saggi interni, salvo diversa indicazione. A una concentrazione di 1 µM, questo composto viene profilato rispetto a un pannello di chinasi utilizzando il kit ProfilerProTM Kinase Selectivity Assay Kit.
In vivo
Linsitinib (OSI-906) inibisce la crescita tumorale in un modello murino di xenotrapianto guidato da IGF-1R, con il 100% di TGI e il 55% di regressione a una dose di 75 mg/kg e il 60% di TGI e nessuna regressione a una dose di 25 mg/kg. La sua somministrazione induce diverse emivite di eliminazione in cane, ratto e topo, che sono rispettivamente di 1,18 ore, 2,64 ore e 2,14 ore. Quando somministrato in diverse dosi singole una volta al giorno in ratti Sprague-Dawley femmine e topi CD-1 femmine, rivela che la Vmax non è dose-proporzionale alla sua dose. Questo composto eleva i livelli di glucosio nel sangue a una dose di 25 mg/kg dopo 12 giorni di somministrazione. A una singola dose di 75 mg/kg in un modello murino di xenotrapianto di IGF-1R umano a lunghezza intera (LISN) guidato da IGF-1R, raggiunge la massima inibizione della fosforilazione di IGF-1R (80%) tra 4 e 24 ore con concentrazioni plasmatiche del farmaco di 26,6-4,77 μM. Quando somministrato come dose singola di 60 mg/kg in topi xenotrapiantati NCI-H292, inibisce l'assorbimento del glucosio a 2, 4 e 24 ore post-trattamento in vivo. Inibisce anche la crescita dei tumori in un modello murino di xenotrapianto NCI-H292.
Riferimenti

Applicazioni (Applications)

Metodi Biomarcatori Immagini PMID
Western blot pS6 / S6 p-STAT3(Y705) / STAT3 pSrc(Y416) / Src cleaved caspase-3 / cleaved PARP p-IGF1R / IGF1R / p-mTOR / mTOR p-EGFR / EGFR / p-IGF1R / IGF1R / p-IRS1 / IRS1 / p-ERK / ERK / p-AKT / AKT
S1091-WB6
21257723
Immunofluorescence FoxO1
S1091-IF1
27535223
Growth inhibition assay Cell viability
S1091-viability1
26136493

Informazioni sullo studio clinico (Clinical Trial Information)

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

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
NCT02546544 Completed
Relapsed Ewing Sarcoma|Refractory Ewing Sarcoma
University of Oxford|European Organisation for Research and Treatment of Cancer - EORTC|European Commission|Astellas Pharma Inc|Oxford University Hospitals NHS Trust
 March 2014 Phase 2
NCT01672736 Terminated
Multiple Myeloma
University Health Network Toronto|Multiple Myeloma Research Consortium|Astellas Pharma Inc
 September 2012 Phase 1|Phase 2
NCT01529684 Completed
Advanced Solid Tumors|Pharmacokinetics of 14C-OSI-906
Astellas Pharma Global Development Inc.|Astellas Pharma Inc
 March 19 2012 Phase 1
NCT01221077 Completed
NSCLC|Non Small Cell Lung Cancer
Astellas Pharma Inc
 April 8 2011 Phase 2

Domande Frequenti (Frequently Asked Questions)

Domanda 1:
Does it dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?

Risposta:
It is a suspension in 30% PEG400/0.5% Tween 80/5% propylene glycol.