Palbociclib (PD-0332991) HCl
中文名称：帕博西尼
Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。Phase 3。
Palbociclib (PD-0332991) HCl Chemical Structure
CAS: 827022-32-2
产品质控
批次：
纯度：
99.99%
99.99
常与Palbociclib (PD-0332991) HCl一起在实验中被使用的化合物
Abemaciclib和Palbociclib HCl是CDK4/6抑制剂，可抑制SARS-CoV-2在AT2和NKX2-5细胞中的复制。
Rudraraju R, et al. Stem Cell Reports. 2023 Jun 13;18(6):1308-1324.
Palbociclib和Ribociclib与内分泌疗法(如芳香化酶抑制剂或氟维司群)联合用于HR阳性、HER2阴性乳腺癌的治疗。
Palbociclib和Olaparib联合用药，对卵巢癌细胞EFO27/OVCAR8/A2780/SNU119/ COV362的生长抑制作用显著增强。
Palbociclib联合Vorinostat可显著抑制CDK4/6-Rb通路激活和HDAC活性，进而降低Cyclin-D1和Bcl-2的表达。
Chaturvedi NK, et al. Leuk Lymphoma. 2019 May;60(5):1214-1223.
Palbociclib和Afatinib联合显著抑制Mcl-1，促进Afatinib耐药细胞PC-9-R/HCC827-R中caspase-3和PARP的切割。
Palbociclib (PD-0332991) HCl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| MCF7 | Function Assay | 0.5-1 μM | 48 h | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MDA-MB-231 | Function Assay | 0.5-1 μM | 48 h | has no Cell cycle arrest assessed as accumulation at sub-G1 phase | 24417566 |
| MCF7 | Function Assay | 1-10 μM | 24 h | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MDA-MB-231 | Function Assay | 1-10 μM | 24 h | does not induce apoptosis assessed as PARP cleavage | 24417566 |
| MDA-MB-231 | Kinase Assay | 5 μM | 24 h | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MCF7 | Kinase Assay | 5 μM | 24 h | Inhibition of recombinant CDK4/cyclinD1 assessed as inhibition of retinoblastoma phosphorylation at Ser780 | 24417566 |
| MCF7 | Growth Inhibition Assay | 1 μM | 24 h | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MDA-MB-231 | Growth Inhibition Assay | 1 μM | 24 h | Cell cycle arrest assessed as accumulation at G1 phase | 24417566 |
| MRC5 | Growth inhibition assay | 72 h | GI50 = 10 μM | 28156111 | |
| DU145 | Cytotoxicity assay | 96 h | IC50 = 7.5 μM | 24417566 | |
| BPH1 | Growth inhibition assay | 72 h | GI50 = 7.442 μM | 28156111 | |
| MDA-MB-468 | Growth inhibition assay | 72 h | GI50 = 5.96 μM | 28156111 | |
| DU145 | Growth inhibition assay | 72 h | GI50 = 5.792 μM | 28156111 | |
| C4-2B | Growth inhibition assay | 72 h | GI50 = 4.15 μM | 28156111 | |
| MDA-MB-468 | Antiproliferative activity assay | 24 h | IC50 = 3 μM | 26115571 | |
| MOLM13 | FLT3 inhibition assay | 24 h | IC50 = 3 μM | 24641103 | |
| M249R | Growth inhibition assay | 72 h | GI50 = 2.96 μM | 28156111 | |
| K562 | Cytotoxicity assay | 96 h | IC50 = 2 μM | 24417566 | |
| M249 | Growth inhibition assay | 72 h | GI50 = 1.99 μM | 28156111 | |
| M238 | Growth inhibition assay | 72 h | GI50 = 1.97 μM | 28156111 | |
| M229 | Growth inhibition assay | 72 h | GI50 = 1.22 μM | 28156111 | |
| MDA-MB-231 | Cytotoxicity assay | 48 h | IC50 = 0.58 μM | 27448913 | |
| MCF7 | Growth inhibition assay | 72 h | GI50 = 0.557 μM | 28156111 | |
| MDA-MB-453 | Growth inhibition assay | 72 h | GI50 = 0.326 μM | 28156111 | |
| MCF7 | Cytotoxicity assay | 48 h | IC50 = 0.24 μM | 27448913 | |
| MDA-MB-435 | Antiproliferative activity assay | 24 h | IC50 = 0.16 μM | 26115571 | |
| U937 | Antiproliferative activity assay | 72 h | IC50 = 0.14 μM | 24641103 | |
| MDA-MB-453 | Cytotoxicity assay | 48 h | IC50 = 0.137 μM | 27448913 | |
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | |
| MOLM13 | Antiproliferative activity assay | 72 h | IC50 = 0.096 μM | 24641103 | |
| PC3 | Growth inhibition assay | 72 h | GI50 = 0.071 μM | 28156111 | |
| NB4 | Growth inhibition assay | 72 h | GI50 = 0.066 μM | 28156111 | |
| MOLM13 | Growth inhibition assay | 72 h | GI50 = 0.062 μM | 28156111 | |
| MV4-11 | Growth inhibition assay | 72 h | GI50 = 0.05 μM | 28156111 | |
| COLO205 | Antiproliferative activity assay | 72 h | IC50 = 0.036 μM | 24641103 | |
| A2780 | Growth inhibition assay | 72 h | GI50 = 0.032 μM | 28156111 | |
| MOLM13 | CDK4 inhibition assay | 24 h | IC50 = 0.011 μM | 24641103 | |
| DU145 | Cytotoxic Assay | 96 h | IC50=7.5 μM | 24417566 | |
| K562 | Cytotoxic Assay | 96 h | IC50=2 μM | 24417566 | |
| MDA-MB-435 | Growth Inhibition Assay | 24 h | IC50=0.16 μM | 15801831 | |
| 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 | |
| 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 | |
| U937 | Growth Inhibition Assay | 72 h | Antiproliferative activity assessed as incorporation of [3H]thymidine into DNA with IC50 of 0.14 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 | |
| MOLM13 | Kinase Assay | 24 h | Inhibition of CDK4 assessed as inhibition of Rb phosphorylation with IC50 of 0.002 μM | 24641103 | |
| NCI-H1573 | Growth Inhibition Assay | IC50=2.07298 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=2.06945 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=2.00666 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=1.99323 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=1.96246 μM | SANGER | ||
| SW872 | Growth Inhibition Assay | IC50=1.9833 μM | SANGER | ||
| G-401 | Growth Inhibition Assay | IC50=1.92428 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=1.91228 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=1.89282 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=1.87412 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=1.81602 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=1.81061 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=1.79542 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=1.78582 μM | SANGER | ||
| CAL-51 | Growth Inhibition Assay | IC50=1.74855 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=1.73212 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=1.70273 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=1.69603 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=1.68061 μM | SANGER | ||
| 22RV1 | Growth Inhibition Assay | IC50=1.67843 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=1.66457 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=1.62152 μM | SANGER | ||
| MG-63 | Growth Inhibition Assay | IC50=1.61813 μM | SANGER | ||
| CAL-62 | Growth Inhibition Assay | IC50=1.60862 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.58507 μM | SANGER | ||
| NCI-H441 | Growth Inhibition Assay | IC50=1.54907 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=1.54071 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=1.50528 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=1.46923 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=1.41774 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=1.37519 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=1.35296 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=1.35221 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=1.32089 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=1.29399 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=1.29338 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=1.26686 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=1.25817 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=1.24267 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=1.22933 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=1.20734 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=1.1862 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=1.17986 μM | SANGER | ||
| CGTH-W-1 | Growth Inhibition Assay | IC50=1.17186 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=1.16354 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.13134 μM | SANGER | ||
| TGW | Growth Inhibition Assay | IC50=1.12395 μM | SANGER | ||
| CHP-134 | Growth Inhibition Assay | IC50=1.11807 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=1.08408 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=1.07522 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=1.07273 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=1.04812 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=1.01421 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=1.00875 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=1.00076 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=998.25 nM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=966.48 nM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=962.81 nM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=940.55 nM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=936.6 nM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=936.06 nM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=929.41 nM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=927.56 nM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=900.1 nM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=897.78 nM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=851.78 nM | SANGER | ||
| CAMA-1 | Growth Inhibition Assay | IC50=833.94 nM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=813.88 nM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=812.79 nM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=808.76 nM | SANGER | ||
| SW962 | Growth Inhibition Assay | IC50=808.63 nM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=778.71 nM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=752.8 nM | SANGER | ||
| NCI-H520 | Growth Inhibition Assay | IC50=746.52 nM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=742.99 nM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=732.27 nM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=728.93 nM | SANGER | ||
| D-263MG | Growth Inhibition Assay | IC50=717.12 nM | SANGER | ||
| KM-H2 | Growth Inhibition Assay | IC50=695.54 nM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=677.82 nM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=652.48 nM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=650.64 nM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=636.99 nM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=633.91 nM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=605.67 nM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=605.21 nM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=603.52 nM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=599.43 nM | SANGER | ||
| NB10 | Growth Inhibition Assay | IC50=599.18 nM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=593.59 nM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=564.99 nM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=526.86 nM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=521.62 nM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=513.85 nM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=509.86 nM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=504.73 nM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=495.43 nM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=494.59 nM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=483.58 nM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=466.9 nM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=444.27 nM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=432.95 nM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=411.89 nM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=405.02 nM | SANGER | ||
| SK-N-AS | Growth Inhibition Assay | IC50=387.83 nM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=376.16 nM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=345.13 nM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=340.66 nM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=321.05 nM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=314.1 nM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=273.09 nM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=258.49 nM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=258.19 nM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=256.25 nM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=252.53 nM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=220.19 nM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=220.02 nM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=198.25 nM | SANGER | ||
| EoL-1 | Growth Inhibition Assay | IC50=187.26 nM | SANGER | ||
| NB69 | Growth Inhibition Assay | IC50=161.8 nM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=96.04 nM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=148.38 nM | 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，无细胞试验中IC50分别为11 nM/16 nM。它对CDK1/2/5，EGFR，FGFR，PDGFR，InsR等没有抑制活性。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | PD-0332991作为有应用前景的工具测定CDK激酶是否具有明显的治疗价值。 | ||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | PD 0332991 对其他蛋白激酶包括EGFR, FGFR, PGFR, IR等没有抑制效果。 PD 0332991作用于Cdk4时是非ATP竞争性抑制剂。PD 0332991抑制MDA-MB-435乳腺癌细胞，IC50为66 nM，是由于Rb 在Ser780的磷酸化作用下降。PD 0332991抑制胸苷合并到Rb阳性的人类乳腺癌，结肠癌 肺癌，及白血病的DNA中，IC50值为4 nM到0.17 μM。PD 0332991作用于Rb阴性细胞没有抑制效果。PD 0332991作用于MDA-MB-453乳腺癌细胞和结肠-205细胞使细胞积累在G1期。[1]PD 0332991也有效作用于骨髓瘤5T33MM细胞，使细胞对Bortezomib敏感。[2]PD 0332991抑制luminalER-阳性和HER2-增强的乳腺癌细胞系，包括MDA-MB-175 ZR-75-30 CAMA-1 MDA-MB-134 HCC-202 UACC-893 等等。在这些细胞系中，PD 0332991增强Tamoxifen和Trastuzumab 的活性。在MCF7抗Tamoxifen细胞中，PD 0332991也增强tamoxifen 的敏感性。[3] 最新研究显示PD 0332991可以抑制恶性横纹肌样肿瘤(MRT)细胞系包括MP-MRT-AN, KP-MRT-RY, G401, KP-MRT-NS，且MRT细胞系对PD 0332991敏感性和p16表达呈负相关。[4] | |||
|---|---|---|---|---|
| 激酶实验 | Cdk实验 | |||
| PD0332991溶解在DMSO中。在96孔板上进行CDK 实验。通过杆状病毒感染，所有的CDK-cyclin 激酶复合体 在昆虫细胞中表达。实验底物为与GST融合的一段pRb。每孔体积为0.1 ml，包含：终浓度为20 mm Tris-HCl（pH 为7.4）, 50 mmNaCl, 1 mm二硫苏糖醇, 10 mmMgCl2, 25 μm ATP (用于CDK4-cyclin D1, CDK6-cyclin D2,和CDK6-cyclin D3)或12 μm ATP (用于CDK2-cyclin E, CDK2-cyclin A, 和CDC2-cyclin B)，0.25 μCi [γ-32P]ATP, 20 ng 酶, 1 μg GST·RB-Cterm, 及PD 0332991 (0.001-0.1μM)。除了[γ-32P]ATP的所有混合物加到孔中，放在搅拌器上搅拌2分钟。加入 [γ-32P]ATP开始反应, 在25 oC下温育15分钟。加入0.1 ml 20% 三氯乙酸终止反应, 在4 oC维持至少1小时，使底物沉淀。用0.2 ml 10%三氯乙酸冲洗5次，用β-计数器板测定掺入的放射性。 | ||||
| 细胞实验 | 细胞系 | MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM，和K562细胞 | ||
| 浓度 | 0.01-1 μM | |||
| 孵育时间 | 24小时 | |||
| 方法 | 肿瘤细胞包括MDA-MB-435, ZR-75-1, T-47D, MCF-7, H1299, Colo-205, MDA-MB-468, H2009, CRRF-CEM，及K562按每孔2×104个细胞接种在96孔板上，温育过夜。加入PD 0332991 (0.01-1 μM) ，37oC温育24小时。每孔加入[14C]胸甘(0.1 μCi) ，进行同位素示踪，持续72小时。用β-计数器板测定掺入的放射性。 |
|||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | 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 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 150 mg/kg PD 0332991处理 MDA-MB-435移植瘤完全抑制肿瘤。在多种人类肿瘤移植瘤中，PD 0332991也显示广谱抗癌活性，通过除去血管中p-Rb和增殖Marker Ki-67，且调节基因使其处于E2F转录水平控制。[1] | |
|---|---|---|
| 动物实验 | Animal Models | 携带晚期人类肿瘤移植瘤，包括结肠-205, MDA-MB-435 乳腺癌, SF-295 恶性胶质瘤, ZR-75-1 乳腺癌, PC-3 前列腺癌, H125 肺癌, SW-620结肠癌, H23肺癌，及MDA-MB-468 乳腺癌 (Rb 阴性)的SCID鼠 |
| Dosages | 0-150 mg/kg | |
| Administration | 口服饲喂 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 | -- |
化学信息&溶解度
| 分子量 | 483.99 | 分子式 | C24H29N7O2.HCl |
| CAS号 | 827022-32-2 | SDF | Download Palbociclib (PD-0332991) HCl SDF |
| Smiles | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
Water : 50 mg/mL (103.3 mM) DMSO : 13 mg/mL ( (26.86 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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