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PD-0332991 (Palbociclib) Hydrochloride CDK4/6 inhibitor

N. Cat.: S1116

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.
PD-0332991 (Palbociclib) Hydrochloride CDK inhibitor Chemical Structure

Struttura chimica

Peso molecolare: 483.99

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.99%
99.99

Prodotti spesso usati con PD-0332991 (Palbociclib) Hydrochloride

SB431542

Explore its induction of SMAD-target genes in T47D cells.

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
MOLM13 Kinase Assay 24 h Inhibition of CDK4 assessed as inhibition of Rb phosphorylation with IC50 of 0.002 μM 24641103
COLO205 Growth Inhibition Assay 72 h Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.036 μM 24641103
U937 Growth Inhibition Assay 72 h Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.14 μM 24641103
MOLM13 Growth Inhibition Assay 72 h Antiproliferative activity against human MOLM13 cells harboring FLT3 ITD mutant assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM 24641103
MOLM13 Growth Inhibition Assay 72 h Antiproliferative activity against sorafenib-resistant human MOLM13 cells assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.096 μM 24641103
MDA-MB-435 Growth Inhibition Assay 24 h IC50=0.16 μM 15801831
K562 Cytotoxic Assay 96 h DMSO IC50=2 μM 24417566
DU145 Cytotoxic Assay 96 h DMSO IC50=7.5 μM 24417566
MDA-MB-231 Growth Inhibition Assay 1 μM 24 h DMSO Cell cycle arrest assessed as accumulation at G1 phase 24417566
MCF7 Growth Inhibition Assay 1 μM 24 h DMSO Cell cycle arrest assessed as accumulation at G1 phase 24417566
MCF7 Kinase Assay 5 μM 24 h DMSO Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 24417566
MDA-MB-231 Kinase Assay 5 μM 24 h DMSO Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 24417566
MDA-MB-231 Function Assay 1-10 μM 24 h DMSO does not induce apoptosis assessed as PARP cleavage 24417566
MCF7 Function Assay 1-10 μM 24 h DMSO does not induce apoptosis assessed as PARP cleavage 24417566
MDA-MB-231 Function Assay 0.5-1 μM 48 h DMSO has no Cell cycle arrest assessed as accumulation at sub-G1 phase 24417566
MCF7 Function Assay 0.5-1 μM 48 h DMSO has no Cell cycle arrest assessed as accumulation at sub-G1 phase 24417566
MOLM13 CDK4 inhibition assay 24 h IC50 = 0.011 μM 24641103
A2780 Growth inhibition assay 72 h GI50 = 0.032 μM 28156111
COLO205 Antiproliferative activity assay 72 h IC50 = 0.036 μM 24641103
MV4-11 Growth inhibition assay 72 h GI50 = 0.05 μM 28156111
MOLM13 Growth inhibition assay 72 h GI50 = 0.062 μM 28156111
NB4 Growth inhibition assay 72 h GI50 = 0.066 μM 28156111
PC3 Growth inhibition assay 72 h GI50 = 0.071 μM 28156111
MOLM13 Antiproliferative activity assay 72 h IC50 = 0.096 μM 24641103
MOLM13 Antiproliferative activity assay 72 h IC50 = 0.096 μM 24641103
MDA-MB-453 Cytotoxicity assay 48 h IC50 = 0.137 μM 27448913
U937 Antiproliferative activity assay 72 h IC50 = 0.14 μM 24641103
MDA-MB-435 Antiproliferative activity assay 24 h IC50 = 0.16 μM 26115571
MCF7 Cytotoxicity assay 48 h IC50 = 0.24 μM 27448913
MDA-MB-453 Growth inhibition assay 72 h GI50 = 0.326 μM 28156111
MCF7 Growth inhibition assay 72 h GI50 = 0.557 μM 28156111
MDA-MB-231 Cytotoxicity assay 48 h IC50 = 0.58 μM 27448913
M229 Growth inhibition assay 72 h GI50 = 1.22 μM 28156111
M238 Growth inhibition assay 72 h GI50 = 1.97 μM 28156111
M249 Growth inhibition assay 72 h GI50 = 1.99 μM 28156111
K562 Cytotoxicity assay 96 h IC50 = 2 μM 24417566
M249R Growth inhibition assay 72 h GI50 = 2.96 μM 28156111
MOLM13 FLT3 inhibition assay 24 h IC50 = 3 μM 24641103
MDA-MB-468 Antiproliferative activity assay 24 h IC50 = 3 μM 26115571
C4-2B Growth inhibition assay 72 h GI50 = 4.15 μM 28156111
DU145 Growth inhibition assay 72 h GI50 = 5.792 μM 28156111
MDA-MB-468 Growth inhibition assay 72 h GI50 = 5.96 μM 28156111
BPH1 Growth inhibition assay 72 h GI50 = 7.442 μM 28156111
DU145 Cytotoxicity assay 96 h IC50 = 7.5 μM 24417566
MRC5 Growth inhibition assay 72 h GI50 = 10 μM 28156111
697 Growth Inhibition Assay IC50=148.38 nM SANGER
P12-ICHIKAWA Growth Inhibition Assay IC50=96.04 nM SANGER
NB69 Growth Inhibition Assay IC50=161.8 nM SANGER
EoL-1 Growth Inhibition Assay IC50=187.26 nM SANGER
BHT-101 Growth Inhibition Assay IC50=198.25 nM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=220.02 nM SANGER
MHH-NB-11 Growth Inhibition Assay IC50=220.19 nM SANGER
AsPC-1 Growth Inhibition Assay IC50=252.53 nM SANGER
ES1 Growth Inhibition Assay IC50=256.25 nM SANGER
LAMA-84 Growth Inhibition Assay IC50=258.19 nM SANGER
MOLT-16 Growth Inhibition Assay IC50=258.49 nM SANGER
ES7 Growth Inhibition Assay IC50=273.09 nM SANGER
KY821 Growth Inhibition Assay IC50=314.1 nM SANGER
RT-112 Growth Inhibition Assay IC50=321.05 nM SANGER
HL-60 Growth Inhibition Assay IC50=340.66 nM SANGER
MOLT-4 Growth Inhibition Assay IC50=345.13 nM SANGER
KARPAS-45 Growth Inhibition Assay IC50=376.16 nM SANGER
SK-N-AS Growth Inhibition Assay IC50=387.83 nM SANGER
CTB-1 Growth Inhibition Assay IC50=405.02 nM SANGER
NKM-1 Growth Inhibition Assay IC50=411.89 nM SANGER
HTC-C3 Growth Inhibition Assay IC50=432.95 nM SANGER
BE-13 Growth Inhibition Assay IC50=444.27 nM SANGER
KOSC-2 Growth Inhibition Assay IC50=466.9 nM SANGER
NB14 Growth Inhibition Assay IC50=483.58 nM SANGER
CAL-27 Growth Inhibition Assay IC50=494.59 nM SANGER
H9 Growth Inhibition Assay IC50=495.43 nM SANGER
RS4-11 Growth Inhibition Assay IC50=504.73 nM SANGER
PA-1 Growth Inhibition Assay IC50=509.86 nM SANGER
MV-4-11 Growth Inhibition Assay IC50=513.85 nM SANGER
OS-RC-2 Growth Inhibition Assay IC50=521.62 nM SANGER
RPMI-8226 Growth Inhibition Assay IC50=526.86 nM SANGER
HGC-27 Growth Inhibition Assay IC50=564.99 nM SANGER
CHP-212 Growth Inhibition Assay IC50=593.59 nM SANGER
NB10 Growth Inhibition Assay IC50=599.18 nM SANGER
HH Growth Inhibition Assay IC50=599.43 nM SANGER
EW-16 Growth Inhibition Assay IC50=603.52 nM SANGER
ES8 Growth Inhibition Assay IC50=605.21 nM SANGER
HAL-01 Growth Inhibition Assay IC50=605.67 nM SANGER
A204 Growth Inhibition Assay IC50=633.91 nM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=636.99 nM SANGER
EM-2 Growth Inhibition Assay IC50=650.64 nM SANGER
BV-173 Growth Inhibition Assay IC50=652.48 nM SANGER
ONS-76 Growth Inhibition Assay IC50=677.82 nM SANGER
KM-H2 Growth Inhibition Assay IC50=695.54 nM SANGER
D-263MG Growth Inhibition Assay IC50=717.12 nM SANGER
ES3 Growth Inhibition Assay IC50=728.93 nM SANGER
VA-ES-BJ Growth Inhibition Assay IC50=732.27 nM SANGER
NBsusSR Growth Inhibition Assay IC50=742.99 nM SANGER
NCI-H520 Growth Inhibition Assay IC50=746.52 nM SANGER
ES5 Growth Inhibition Assay IC50=752.8 nM SANGER
T-24 Growth Inhibition Assay IC50=778.71 nM SANGER
SW962 Growth Inhibition Assay IC50=808.63 nM SANGER
EW-3 Growth Inhibition Assay IC50=808.76 nM SANGER
RXF393 Growth Inhibition Assay IC50=812.79 nM SANGER
U251 Growth Inhibition Assay IC50=813.88 nM SANGER
CAMA-1 Growth Inhibition Assay IC50=833.94 nM SANGER
JVM-3 Growth Inhibition Assay IC50=851.78 nM SANGER
COLO-800 Growth Inhibition Assay IC50=897.78 nM SANGER
OVCAR-5 Growth Inhibition Assay IC50=900.1 nM SANGER
LB1047-RCC Growth Inhibition Assay IC50=927.56 nM SANGER
SW954 Growth Inhibition Assay IC50=929.41 nM SANGER
J-RT3-T3-5 Growth Inhibition Assay IC50=936.06 nM SANGER
Mewo Growth Inhibition Assay IC50=936.6 nM SANGER
NCI-H1770 Growth Inhibition Assay IC50=940.55 nM SANGER
HO-1-N-1 Growth Inhibition Assay IC50=962.81 nM SANGER
HSC-3 Growth Inhibition Assay IC50=966.48 nM SANGER
TYK-nu Growth Inhibition Assay IC50=998.25 nM SANGER
KYSE-150 Growth Inhibition Assay IC50=1.00076 μM SANGER
SN12C Growth Inhibition Assay IC50=1.00875 μM SANGER
MOLT-13 Growth Inhibition Assay IC50=1.01421 μM SANGER
TE-11 Growth Inhibition Assay IC50=1.04812 μM SANGER
DB Growth Inhibition Assay IC50=1.07273 μM SANGER
CAL-39 Growth Inhibition Assay IC50=1.07522 μM SANGER
A3-KAW Growth Inhibition Assay IC50=1.08408 μM SANGER
CHP-134 Growth Inhibition Assay IC50=1.11807 μM SANGER
TGW Growth Inhibition Assay IC50=1.12395 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=1.13134 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=1.16354 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=1.17186 μM SANGER
MHH-ES-1 Growth Inhibition Assay IC50=1.17986 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=1.1862 μM SANGER
ML-2 Growth Inhibition Assay IC50=1.20734 μM SANGER
COR-L23 Growth Inhibition Assay IC50=1.22933 μM SANGER
BFTC-905 Growth Inhibition Assay IC50=1.24267 μM SANGER
Hs-578-T Growth Inhibition Assay IC50=1.25817 μM SANGER
KG-1 Growth Inhibition Assay IC50=1.26686 μM SANGER
HEL Growth Inhibition Assay IC50=1.29338 μM SANGER
A549 Growth Inhibition Assay IC50=1.29399 μM SANGER
COLO-741 Growth Inhibition Assay IC50=1.32089 μM SANGER
PC-3 Growth Inhibition Assay IC50=1.35221 μM SANGER
HOS Growth Inhibition Assay IC50=1.35296 μM SANGER
HT-1080 Growth Inhibition Assay IC50=1.37519 μM SANGER
TE-8 Growth Inhibition Assay IC50=1.41774 μM SANGER
BHY Growth Inhibition Assay IC50=1.46923 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=1.50528 μM SANGER
HN Growth Inhibition Assay IC50=1.54071 μM SANGER
NCI-H441 Growth Inhibition Assay IC50=1.54907 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=1.58507 μM SANGER
CAL-62 Growth Inhibition Assay IC50=1.60862 μM SANGER
MG-63 Growth Inhibition Assay IC50=1.61813 μM SANGER
SK-LU-1 Growth Inhibition Assay IC50=1.62152 μM SANGER
BCPAP Growth Inhibition Assay IC50=1.66457 μM SANGER
22RV1 Growth Inhibition Assay IC50=1.67843 μM SANGER
T47D Growth Inhibition Assay IC50=1.68061 μM SANGER
MSTO-211H Growth Inhibition Assay IC50=1.69603 μM SANGER
DEL Growth Inhibition Assay IC50=1.70273 μM SANGER
H4 Growth Inhibition Assay IC50=1.73212 μM SANGER
CAL-51 Growth Inhibition Assay IC50=1.74855 μM SANGER
ABC-1 Growth Inhibition Assay IC50=1.78582 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=1.79542 μM SANGER
YKG-1 Growth Inhibition Assay IC50=1.81061 μM SANGER
KM12 Growth Inhibition Assay IC50=1.81602 μM SANGER
L-363 Growth Inhibition Assay IC50=1.87412 μM SANGER
KU812 Growth Inhibition Assay IC50=1.89282 μM SANGER
LOXIMVI Growth Inhibition Assay IC50=1.91228 μM SANGER
G-401 Growth Inhibition Assay IC50=1.92428 μM SANGER
SW780 Growth Inhibition Assay IC50=1.96246 μM SANGER
SW872 Growth Inhibition Assay IC50=1.9833 μM SANGER
NB7 Growth Inhibition Assay IC50=1.99323 μM SANGER
T98G Growth Inhibition Assay IC50=2.00666 μM SANGER
SW1710 Growth Inhibition Assay IC50=2.06945 μM SANGER
NCI-H1573 Growth Inhibition Assay IC50=2.07298 μM SANGER
KE-37 Growth Inhibition Assay IC50=2.08951 μM SANGER
786-0 Growth Inhibition Assay IC50=2.15439 μM SANGER
SAS Growth Inhibition Assay IC50=2.20374 μM SANGER
CAL-54 Growth Inhibition Assay IC50=2.20413 μM SANGER
SF268 Growth Inhibition Assay IC50=2.23122 μM SANGER
SW620 Growth Inhibition Assay IC50=2.26169 μM SANGER
MN-60 Growth Inhibition Assay IC50=2.3106 μM SANGER
EFO-27 Growth Inhibition Assay IC50=2.32058 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=2.32199 μM SANGER
HCC2218 Growth Inhibition Assay IC50=2.35374 μM SANGER
MIA-PaCa-2 Growth Inhibition Assay IC50=2.36437 μM SANGER
SJSA-1 Growth Inhibition Assay IC50=2.37796 μM SANGER
RKO Growth Inhibition Assay IC50=2.38496 μM SANGER
NB6 Growth Inhibition Assay IC50=2.40374 μM SANGER
ES4 Growth Inhibition Assay IC50=2.45422 μM SANGER
EGI-1 Growth Inhibition Assay IC50=2.46883 μM SANGER
CTV-1 Growth Inhibition Assay IC50=2.52773 μM SANGER
NCI-H1355 Growth Inhibition Assay IC50=2.55951 μM SANGER
GT3TKB Growth Inhibition Assay IC50=2.59199 μM SANGER
SK-HEP-1 Growth Inhibition Assay IC50=2.59266 μM SANGER
GAMG Growth Inhibition Assay IC50=2.59394 μM SANGER
SK-MES-1 Growth Inhibition Assay IC50=2.61803 μM SANGER
RO82-W-1 Growth Inhibition Assay IC50=2.62057 μM SANGER
ECC10 Growth Inhibition Assay IC50=2.70206 μM SANGER
MCF7 Growth Inhibition Assay IC50=2.71464 μM SANGER
D-283MED Growth Inhibition Assay IC50=2.7243 μM SANGER
RPMI-7951 Growth Inhibition Assay IC50=2.75694 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=2.77099 μM SANGER
KGN Growth Inhibition Assay IC50=2.81884 μM SANGER
NUGC-3 Growth Inhibition Assay IC50=2.82505 μM SANGER
NCI-H292 Growth Inhibition Assay IC50=2.85053 μM SANGER
Becker Growth Inhibition Assay IC50=2.95832 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=3.05263 μM SANGER
ETK-1 Growth Inhibition Assay IC50=3.0543 μM SANGER
TK10 Growth Inhibition Assay IC50=3.20165 μM SANGER
VMRC-RCZ Growth Inhibition Assay IC50=3.36488 μM SANGER
YH-13 Growth Inhibition Assay IC50=3.44079 μM SANGER
DU-145 Growth Inhibition Assay IC50=3.46269 μM SANGER
SW1088 Growth Inhibition Assay IC50=3.4747 μM SANGER
HOP-92 Growth Inhibition Assay IC50=3.50342 μM SANGER
KP-N-YS Growth Inhibition Assay IC50=3.62139 μM SANGER
NCI-H460 Growth Inhibition Assay IC50=3.6673 μM SANGER
U-2-OS Growth Inhibition Assay IC50=3.72535 μM SANGER
A101D Growth Inhibition Assay IC50=3.76936 μM SANGER
MDA-MB-231 Growth Inhibition Assay IC50=3.81951 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=3.832 μM SANGER
COR-L105 Growth Inhibition Assay IC50=4.018 μM SANGER
NCI-H1437 Growth Inhibition Assay IC50=4.02302 μM SANGER
CAL-85-1 Growth Inhibition Assay IC50=4.02461 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=4.18556 μM SANGER
VM-CUB-1 Growth Inhibition Assay IC50=4.31284 μM SANGER
CHL-1 Growth Inhibition Assay IC50=4.32169 μM SANGER
MDA-MB-361 Growth Inhibition Assay IC50=4.33153 μM SANGER
NCI-H661 Growth Inhibition Assay IC50=4.50092 μM SANGER
EW-11 Growth Inhibition Assay IC50=4.52231 μM SANGER
BEN Growth Inhibition Assay IC50=4.52815 μM SANGER
BFTC-909 Growth Inhibition Assay IC50=4.56275 μM SANGER
NCI-H2087 Growth Inhibition Assay IC50=4.58164 μM SANGER
RVH-421 Growth Inhibition Assay IC50=4.6669 μM SANGER
P30-OHK Growth Inhibition Assay IC50=4.68008 μM SANGER
NCI-H28 Growth Inhibition Assay IC50=4.81661 μM SANGER
ES6 Growth Inhibition Assay IC50=4.83016 μM SANGER
769-P Growth Inhibition Assay IC50=4.85926 μM SANGER
OE33 Growth Inhibition Assay IC50=4.88161 μM SANGER
SW982 Growth Inhibition Assay IC50=4.95061 μM SANGER
A388 Growth Inhibition Assay IC50=5.02983 μM SANGER
TI-73 Growth Inhibition Assay IC50=5.06194 μM SANGER
HCT-116 Growth Inhibition Assay IC50=5.09889 μM SANGER
HuP-T3 Growth Inhibition Assay IC50=5.18709 μM SANGER
G-402 Growth Inhibition Assay IC50=5.19416 μM SANGER
NCI-H1792 Growth Inhibition Assay IC50=5.24622 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=5.25942 μM SANGER
NCI-H1650 Growth Inhibition Assay IC50=5.30634 μM SANGER
LCLC-97TM1 Growth Inhibition Assay IC50=5.31808 μM SANGER
S-117 Growth Inhibition Assay IC50=5.36976 μM SANGER
GI-ME-N Growth Inhibition Assay IC50=5.39681 μM SANGER
NCI-H2122 Growth Inhibition Assay IC50=5.49397 μM SANGER
NCI-H1793 Growth Inhibition Assay IC50=5.67593 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=5.70088 μM SANGER
TE-12 Growth Inhibition Assay IC50=5.80556 μM SANGER
LCLC-103H Growth Inhibition Assay IC50=5.917 μM SANGER
A673 Growth Inhibition Assay IC50=5.91932 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=5.9836 μM SANGER
SF295 Growth Inhibition Assay IC50=6.00422 μM SANGER
KU-19-19 Growth Inhibition Assay IC50=6.01731 μM SANGER
CFPAC-1 Growth Inhibition Assay IC50=6.04443 μM SANGER
LoVo Growth Inhibition Assay IC50=6.05063 μM SANGER
8505C Growth Inhibition Assay IC50=6.07573 μM SANGER
GMS-10 Growth Inhibition Assay IC50=6.15002 μM SANGER
Ca9-22 Growth Inhibition Assay IC50=6.1671 μM SANGER
DOK Growth Inhibition Assay IC50=6.22072 μM SANGER
FADU Growth Inhibition Assay IC50=6.26039 μM SANGER
BxPC-3 Growth Inhibition Assay IC50=6.2732 μM SANGER
CAL-33 Growth Inhibition Assay IC50=6.29201 μM SANGER
SHP-77 Growth Inhibition Assay IC50=6.31512 μM SANGER
LXF-289 Growth Inhibition Assay IC50=6.33455 μM SANGER
GB-1 Growth Inhibition Assay IC50=6.382 μM SANGER
KS-1 Growth Inhibition Assay IC50=6.38447 μM SANGER
D-502MG Growth Inhibition Assay IC50=6.42376 μM SANGER
LAN-6 Growth Inhibition Assay IC50=6.51023 μM SANGER
H-EMC-SS Growth Inhibition Assay IC50=6.56147 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=6.60076 μM SANGER
NCI-H1693 Growth Inhibition Assay IC50=6.62215 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=6.75044 μM SANGER
D-423MG Growth Inhibition Assay IC50=6.76117 μM SANGER
KNS-42 Growth Inhibition Assay IC50=6.78197 μM SANGER
GCT Growth Inhibition Assay IC50=6.938 μM SANGER
DSH1 Growth Inhibition Assay IC50=7.0633 μM SANGER
D-247MG Growth Inhibition Assay IC50=7.07881 μM SANGER
NCI-SNU-5 Growth Inhibition Assay IC50=7.18371 μM SANGER
TE-6 Growth Inhibition Assay IC50=7.20601 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=7.22127 μM SANGER
NB17 Growth Inhibition Assay IC50=7.30309 μM SANGER
EW-22 Growth Inhibition Assay IC50=7.34348 μM SANGER
EW-13 Growth Inhibition Assay IC50=7.35162 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=7.4402 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=7.49899 μM SANGER
GR-ST Growth Inhibition Assay IC50=7.52594 μM SANGER
KYSE-520 Growth Inhibition Assay IC50=7.55515 μM SANGER
CAPAN-1 Growth Inhibition Assay IC50=7.5951 μM SANGER
HCE-4 Growth Inhibition Assay IC50=7.62279 μM SANGER
MLMA Growth Inhibition Assay IC50=7.62957 μM SANGER
HT-144 Growth Inhibition Assay IC50=7.65368 μM SANGER
KYSE-180 Growth Inhibition Assay IC50=7.71169 μM SANGER
TE-5 Growth Inhibition Assay IC50=7.95971 μM SANGER
IGROV-1 Growth Inhibition Assay IC50=7.98551 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=8.012 μM SANGER
SW1990 Growth Inhibition Assay IC50=8.04659 μM SANGER
EFM-19 Growth Inhibition Assay IC50=8.08545 μM SANGER
OGR-1 Growth Inhibition Assay IC50=8.43023 μM SANGER
U-118-MG Growth Inhibition Assay IC50=8.43463 μM SANGER
SK-OV-3 Growth Inhibition Assay IC50=8.46765 μM SANGER
KNS-62 Growth Inhibition Assay IC50=8.51761 μM SANGER
GOTO Growth Inhibition Assay IC50=8.57635 μM SANGER
8305C Growth Inhibition Assay IC50=8.70484 μM SANGER
RPMI-2650 Growth Inhibition Assay IC50=8.71955 μM SANGER
NEC8 Growth Inhibition Assay IC50=8.74307 μM SANGER
KYSE-450 Growth Inhibition Assay IC50=8.86548 μM SANGER
RMG-I Growth Inhibition Assay IC50=9.14058 μM SANGER
CAKI-1 Growth Inhibition Assay IC50=9.31979 μM SANGER
KYSE-510 Growth Inhibition Assay IC50=9.35778 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=9.36701 μM SANGER
AN3-CA Growth Inhibition Assay IC50=9.45444 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=9.72849 μM SANGER
HSC-2 Growth Inhibition Assay IC50=9.76629 μM SANGER
EW-1 Growth Inhibition Assay IC50=9.79369 μM SANGER
D-566MG Growth Inhibition Assay IC50=9.83664 μM SANGER
COLO-792 Growth Inhibition Assay IC50=9.98746 μM SANGER
TE-10 Growth Inhibition Assay IC50=10.0396 μM SANGER
NCI-H650 Growth Inhibition Assay IC50=10.4286 μM SANGER
U-266 Growth Inhibition Assay IC50=10.455 μM SANGER
Detroit562 Growth Inhibition Assay IC50=11.0515 μM SANGER
NH-12 Growth Inhibition Assay IC50=11.1446 μM SANGER
CO-314 Growth Inhibition Assay IC50=11.2842 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=11.5323 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=11.5527 μM SANGER
SW1463 Growth Inhibition Assay IC50=11.5989 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=11.6552 μM SANGER
SK-MEL-2 Growth Inhibition Assay IC50=11.7197 μM SANGER
NB13 Growth Inhibition Assay IC50=12.1495 μM SANGER
Daoy Growth Inhibition Assay IC50=12.2856 μM SANGER
NCI-H1623 Growth Inhibition Assay IC50=12.3801 μM SANGER
NMC-G1 Growth Inhibition Assay IC50=12.717 μM SANGER
DK-MG Growth Inhibition Assay IC50=12.9482 μM SANGER
TCCSUP Growth Inhibition Assay IC50=13.1284 μM SANGER
SCC-15 Growth Inhibition Assay IC50=13.2651 μM SANGER
NOS-1 Growth Inhibition Assay IC50=13.2893 μM SANGER
RH-1 Growth Inhibition Assay IC50=13.3037 μM SANGER
SK-MEL-3 Growth Inhibition Assay IC50=13.3728 μM SANGER
NB5 Growth Inhibition Assay IC50=13.4067 μM SANGER
SNU-387 Growth Inhibition Assay IC50=13.5072 μM SANGER
CAL-120 Growth Inhibition Assay IC50=13.6718 μM SANGER
Mo-T Growth Inhibition Assay IC50=13.707 μM SANGER
LNCaP-Clone-FGC Growth Inhibition Assay IC50=13.7992 μM SANGER
CAN Growth Inhibition Assay IC50=14.0288 μM SANGER
SK-MEL-30 Growth Inhibition Assay IC50=14.063 μM SANGER
COLO-678 Growth Inhibition Assay IC50=14.0822 μM SANGER
SCC-9 Growth Inhibition Assay IC50=14.1021 μM SANGER
KINGS-1 Growth Inhibition Assay IC50=14.1402 μM SANGER
SL-513 Growth Inhibition Assay IC50=14.187 μM SANGER
HLE Growth Inhibition Assay IC50=14.3852 μM SANGER
SW1573 Growth Inhibition Assay IC50=14.4435 μM SANGER
KYSE-140 Growth Inhibition Assay IC50=14.6327 μM SANGER
SK-PN-DW Growth Inhibition Assay IC50=14.8001 μM SANGER
A253 Growth Inhibition Assay IC50=15.0625 μM SANGER
CAL-12T Growth Inhibition Assay IC50=15.4662 μM SANGER
COLO-679 Growth Inhibition Assay IC50=15.7683 μM SANGER
UACC-257 Growth Inhibition Assay IC50=16.1201 μM SANGER
U-87-MG Growth Inhibition Assay IC50=16.3523 μM SANGER
HCC1806 Growth Inhibition Assay IC50=16.7071 μM SANGER
NCI-H2170 Growth Inhibition Assay IC50=17.2448 μM SANGER
AGS Growth Inhibition Assay IC50=17.3808 μM SANGER
MEL-HO Growth Inhibition Assay IC50=17.7503 μM SANGER
SW48 Growth Inhibition Assay IC50=17.7716 μM SANGER
HuP-T4 Growth Inhibition Assay IC50=18.0206 μM SANGER
NCI-H720 Growth Inhibition Assay IC50=18.1402 μM SANGER
RCC10RGB Growth Inhibition Assay IC50=18.1697 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=18.2254 μM SANGER
A427 Growth Inhibition Assay IC50=18.5094 μM SANGER
HCC2998 Growth Inhibition Assay IC50=18.6051 μM SANGER
EPLC-272H Growth Inhibition Assay IC50=19.0434 μM SANGER
C32 Growth Inhibition Assay IC50=19.045 μM SANGER
UMC-11 Growth Inhibition Assay IC50=19.2123 μM SANGER
CaR-1 Growth Inhibition Assay IC50=19.6804 μM SANGER
KYSE-410 Growth Inhibition Assay IC50=19.9139 μM SANGER
HuCCT1 Growth Inhibition Assay IC50=20.6294 μM SANGER
LB996-RCC Growth Inhibition Assay IC50=20.7168 μM SANGER
KYSE-70 Growth Inhibition Assay IC50=20.8059 μM SANGER
CAL-72 Growth Inhibition Assay IC50=20.915 μM SANGER
Capan-2 Growth Inhibition Assay IC50=21.0413 μM SANGER
PANC-08-13 Growth Inhibition Assay IC50=21.2515 μM SANGER
SBC-1 Growth Inhibition Assay IC50=21.3081 μM SANGER
MFM-223 Growth Inhibition Assay IC50=21.3342 μM SANGER
BB49-HNC Growth Inhibition Assay IC50=21.5716 μM SANGER
SH-4 Growth Inhibition Assay IC50=21.6618 μM SANGER
HuO9 Growth Inhibition Assay IC50=21.9825 μM SANGER
AM-38 Growth Inhibition Assay IC50=22.0485 μM SANGER
A431 Growth Inhibition Assay IC50=23.2119 μM SANGER
YAPC Growth Inhibition Assay IC50=23.2651 μM SANGER
LU-139 Growth Inhibition Assay IC50=23.4809 μM SANGER
HEC-1 Growth Inhibition Assay IC50=23.4937 μM SANGER
SCC-25 Growth Inhibition Assay IC50=24.3006 μM SANGER
HT-29 Growth Inhibition Assay IC50=24.3823 μM SANGER
PC-14 Growth Inhibition Assay IC50=24.6571 μM SANGER
Calu-6 Growth Inhibition Assay IC50=25.5071 μM SANGER
SJRH30 Growth Inhibition Assay IC50=25.6496 μM SANGER
ChaGo-K-1 Growth Inhibition Assay IC50=26.1629 μM SANGER
IA-LM Growth Inhibition Assay IC50=26.3645 μM SANGER
GP5d Growth Inhibition Assay IC50=26.4491 μM SANGER
NCI-H2291 Growth Inhibition Assay IC50=26.6541 μM SANGER
BALL-1 Growth Inhibition Assay IC50=26.9397 μM SANGER
HCC1954 Growth Inhibition Assay IC50=26.9808 μM SANGER
NCI-H2452 Growth Inhibition Assay IC50=27.4163 μM SANGER
LU-99A Growth Inhibition Assay IC50=27.5582 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=27.7299 μM SANGER
PANC-10-05 Growth Inhibition Assay IC50=27.7775 μM SANGER
NCI-H2405 Growth Inhibition Assay IC50=27.9387 μM SANGER
MDA-MB-415 Growth Inhibition Assay IC50=28.4137 μM SANGER
NCI-H2342 Growth Inhibition Assay IC50=28.5281 μM SANGER
TGBC24TKB Growth Inhibition Assay IC50=28.7117 μM SANGER
LU-134-A Growth Inhibition Assay IC50=28.9261 μM SANGER
SCC-4 Growth Inhibition Assay IC50=31.0494 μM SANGER
Saos-2 Growth Inhibition Assay IC50=31.9306 μM SANGER
RERF-LC-MS Growth Inhibition Assay IC50=32.8231 μM SANGER
M14 Growth Inhibition Assay IC50=32.9764 μM SANGER
HPAF-II Growth Inhibition Assay IC50=33.5011 μM SANGER
NCI-H1755 Growth Inhibition Assay IC50=34.3305 μM SANGER
D-392MG Growth Inhibition Assay IC50=35.8674 μM SANGER
A704 Growth Inhibition Assay IC50=36.0427 μM SANGER
CP50-MEL-B Growth Inhibition Assay IC50=36.1911 μM SANGER
EW-18 Growth Inhibition Assay IC50=36.452 μM SANGER
WM-115 Growth Inhibition Assay IC50=36.8099 μM SANGER
LU-65 Growth Inhibition Assay IC50=37.1417 μM SANGER
NCI-H1563 Growth Inhibition Assay IC50=37.2484 μM SANGER
DBTRG-05MG Growth Inhibition Assay IC50=38.0691 μM SANGER
NCI-H630 Growth Inhibition Assay IC50=38.4714 μM SANGER
NCI-H1155 Growth Inhibition Assay IC50=39.242 μM SANGER
OVACR-3 Growth Inhibition Assay IC50=39.9195 μM SANGER
OAW-42 Growth Inhibition Assay IC50=40.4258 μM SANGER
JVM-2 Growth Inhibition Assay IC50=41.2415 μM SANGER
C3A Growth Inhibition Assay IC50=41.3447 μM SANGER
HT55 Growth Inhibition Assay IC50=42.2841 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=42.2974 μM SANGER
MEG-01 Growth Inhibition Assay IC50=42.4616 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=43.9892 μM SANGER
JEG-3 Growth Inhibition Assay IC50=44.947 μM SANGER
BPH-1 Growth Inhibition Assay IC50=46.3998 μM SANGER
MPP-89 Growth Inhibition Assay IC50=47.2898 μM SANGER
ALL-PO Growth Inhibition Assay IC50=47.4188 μM SANGER
HT Growth Inhibition Assay IC50=47.492 μM SANGER
NCI-H2347 Growth Inhibition Assay IC50=48.0715 μM SANGER
A2780 Growth Inhibition Assay IC50=49.4228 μM SANGER
KARPAS-299 Growth Inhibition Assay IC50=49.5119 μM SANGER
NCI-H1651 Growth Inhibition Assay IC50=49.8821 μM SANGER
Clicca per visualizzare più dati sperimentali sulle linee cellulari

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

Peso molecolare 483.99 Formula

C24H29N7O2.HCl

 Conservazione (Dalla data di ricezione)
N. CAS 827022-32-2 Scarica SDF Conservazione delle soluzioni stock

Sinonimi N/A Smiles CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl

Solubilità (Solubility)

In vitro
Lotto:

Water : 50 mg/mL

DMSO : 13 mg/mL (26.86 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

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)

Caratteristiche
Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Targets/IC50/Ki
CDK4/CyclinD3
(Cell-free assay)
9 nM
CDK4/CyclinD1
(Cell-free assay)
11 nM
CDK6/CyclinD2
(Cell-free assay)
15 nM
In vitro
PD 0332991 ha scarso effetto su altre chinasi proteiche tra cui EGFR, FGFR, PGFR, IR. PD 0332991 è un inibitore non competitivo dell'ATP di Cdk4. PD 0332991 inibisce le cellule di carcinoma mammario MDA-MB-435 con IC50 di 66 nM, il che è dovuto a una ridotta fosforilazione di Rb a Ser780. PD 0332991 inibisce l'incorporazione di timidina nel DNA di carcinomi mammari, del colon e polmonari umani Rb-positivi, nonché leucemie umane, con valori di IC50 compresi tra 0,04-0,17 μM. PD 0332991 non mostra attività nelle cellule Rb-negative. PD 0332991 provoca un accumulo di cellule in G1 nelle cellule mammarie MDA-MB-453 e nelle cellule di carcinoma Colo-205. PD 0332991 mostra anche attività nelle cellule di mieloma 5T33MM (modello immunocompetente) e sensibilizza le cellule all'uccisione da bortezomib. PD 0332991 inibisce le linee cellulari di cancro al seno luminali ER-positive e HER2-amplificate, tra cui MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 e UACC-893. PD 0332991 aumenta l'attività di tamoxifene e trastuzumab in queste linee cellulari. PD 0332991 aumenta la sensibilità del tamoxifene nelle cellule MCF7 resistenti al tamoxifene. Uno studio recente mostra che PD 0332991 potrebbe sopprimere le linee cellulari di tumore rabdoide maligno (MRT) tra cui MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS e la sensibilità delle linee cellulari MRT a PD 0332991 è inversamente correlata all'espressione di p16.
Saggio chinasico
Saggi Cdk
Una soluzione madre di PD0332991 viene preparata in DMSO. I saggi CDK vengono eseguiti in piastre di filtrazione a 96 pozzetti. Tutti i complessi chinasi CDK-ciclina sono espressi in cellule di insetto tramite infezione da baculovirus e purificati. Il substrato per i saggi è un frammento (aminoacidi 792–928) di pRb fuso a GST (GST·RB-Cterm). Il volume totale in ogni pozzetto è di 0,1 mL contenente una concentrazione finale di 20 mM Tris-HCl, pH 7,4, 50 mM NaCl, 1 mM ditiotreitolo, 10 mM MgCl2, 25 μM ATP (per CDK4-ciclina D1, CDK6-ciclina D2 e CDK6-ciclina D3) o 12 μM ATP (per CDK2-ciclina E, CDK2-ciclina A e CDC2-ciclina B) contenente 0,25 μCi di [γ-32P]ATP, 20 ng di enzima, 1 μg di GST·RB-Cterm e PD 0332991 (0,001-0,1μM). Tutti i componenti tranne il [γ-32P]ATP vengono aggiunti ai pozzetti, e la piastra viene posta su un miscelatore di piastre per 2 minuti. La reazione viene avviata aggiungendo il [γ-32P]ATP e la piastra viene incubata a 25 °C per 15 minuti. La reazione viene terminata con l'aggiunta di 0,1 mL di acido tricloroacetico al 20% e la piastra viene mantenuta a 4 °C per almeno 1 ora per consentire al substrato di precipitare. I pozzetti vengono quindi lavati 5 volte con 0,2 mL di acido tricloroacetico al 10% e l'incorporazione radioattiva viene determinata con un contatore di piastre β.
In vivo
Il PD 0332991 indica una stasi tumorale completa in uno xenotrapianto MDA-MB-435 a 150 mg/kg. Il PD 0332991 mostra anche un'attività antitumorale ad ampio spettro in molteplici xenotrapianti tumorali umani eliminando il phospho-Rb e il marker proliferativo Ki-67 dal tessuto tumorale e la down-regulation dei geni sotto il controllo trascrizionale di E2F.
Riferimenti
  • [4] https://pubmed.ncbi.nlm.nih.gov/21871868/

Applicazioni (Applications)

Metodi Biomarcatori Immagini PMID
Western blot RB1 (pT821) / RB1 (pS780) / RB1 / CDK6 / CCND2 / RUNX1 / ETO pRb(S807, 811) / CDK4 / CDK6 / PARP LC3-I / LC3-II pAMPKα(T172) / pULK1(S317) SMAD2 (pS255)
S1116-WB1
30300583
Growth inhibition assay Cell viability
S1116-viability1
29670090
Immunofluorescence SAHF/ATRX LC3B
S1116-IF1
26988987
ELISA PGE2
S1116-ELISA1
26540629

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
NCT05665361 Recruiting
Advanced Clear Cell Renal Carcinoma (Ccrcc)|Papillary Renal Cell Carcinoma (Prcc)
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 April 24 2024 Phase 1|Phase 2
NCT06307457 Completed
Breast Cancer
Pfizer
 March 11 2024 --
NCT05912933 Not yet recruiting
Breast Cancer
Pfizer
 March 1 2024 --
NCT05709158 Not yet recruiting
Breast Cancer
Pfizer
 March 1 2024 --