연구용
PD-0332991 (Palbociclib) Hydrochloride CDK4/6 inhibitor
제품 번호: S1116
화학 구조
분자량: 483.99
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품질 관리 (Quality Control)
배치:
순도:
99.99%
99.99
함께 자주 사용되는 제품 PD-0332991 (Palbociclib) Hydrochloride
세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | 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 | |||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)
| 분자량 | 483.99 | 화학식 | C24H29N7O2.HCl |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 827022-32-2 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | N/A | Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl | ||
용해도 (Solubility)
|
In vitro |
Water : 50 mg/mL
DMSO
: 13 mg/mL
(26.86 mM)
Ethanol : Insoluble |
몰농도 계산기
희석 계산기
분자량 계산기
|
In vivo |
|||||
생체 내 제형 계산기 (투명한 용액)
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
mg/kg
g
μL
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
작용 메커니즘 (Mechanism of Action)
| 특징 |
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
|
| 시험관 내(In vitro) |
PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells with IC50 of 66 nM, which is due to reduced Rb phosphorylation at Ser780. PD 0332991 inhibits thymidine incorporation into the DNA of Rb-positive human breast, colon, and lung carcinomas as well as human leukemias, with IC50 values ranging from 0.04-0.17 μM. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 causes an accumulation of cells in G1 in MDA-MB-453 breast and Colo-205 carcinoma cells. PD 0332991 also shows activity in 5T33MM myeloma cells (immunocompetent model) and sensitizes the cells to killing by bortezomib. PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines including MDA-MB-175, ZR-75-30, CAMA-1, MDA-MB-134, HCC-202 and UACC-893. PD 0332991 enhances the activity of tamoxifen and trastuzumab in these cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. A recent study shows that PD 0332991 could suppress malignant rhabdoid tumor (MRT) cell lines including MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS and the sensitivity of the MRT cell lines to PD 0332991 is inversely correlated with expression of p16.
|
| 키나아제 분석 |
Cdk Assays
|
|
A stock solution of PD0332991 is prepared in DMSO. CDK assays are performed in 96-well filter plates. All CDK-cyclin kinase complexes are expressed in insect cells through baculovirus infection and purified. The substrate for the assays is a fragment (amino acids 792–928) of pRb fused to GST (GST·RB-Cterm). The total volume in each well is 0.1 mL containing a final concentration of 20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM dithiothreitol, 10 mM MgCl2, 25 μM ATP (for CDK4-cyclin D1, CDK6-cyclin D2, and CDK6-cyclin D3) or 12 μM ATP (for CDK2-cyclin E, CDK2-cyclin A, and CDC2-cyclin B) containing 0.25 μCi of [γ-32P]ATP, 20 ng of enzyme, 1 μg of GST·RB-Cterm, and PD 0332991 (0.001-0.1μM). All components except the [γ-32P]ATP are added to the wells, and the plate is placed on a plate mixer for 2 min. The reaction is started by adding the [γ-32P]ATP and the plate is incubated at 25 °C for 15 min. The reaction is terminated by addition of 0.1 mL of 20% trichloroacetic acid and the plate is kept at 4 °C for at least 1 hour to allow the substrate to precipitate. The wells are then washed 5 times with 0.2 mL of 10% trichloroacetic acid and radioactive incorporation is determined with a β plate counter.
|
|
| 생체 내(In vivo) |
PD 0332991 indicates complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg. PD 0332991 also shows broad-spectrum antitumor activity in multiple human tumor xenografts by eliminating phospho-Rb and the proliferative marker Ki-67 from tumor tissue and down-regulation of genes under the transcriptional control of E2F.
|
참조 |
|
적용 분야 (Applications)
| 방법 | 바이오마커 | 이미지 | 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) |
|
30300583 |
| Growth inhibition assay | Cell viability |
|
29670090 |
| Immunofluorescence | SAHF/ATRX LC3B |
|
26988987 |
| ELISA | PGE2 |
|
26540629 |
임상시험 정보 (Clinical Trial Information)
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| 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 | -- |
제품은 연구용으로만 사용됩니다. 인체에는 사용하지 마십시오. 환자에게 판매하지 않습니다.
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