| 应用 |
A highly selective inhibitor of Cdk4/cyclin D1 and Cdk6/cyclin D2. |
| 产品介绍 |
Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂，IC50为11 nM/16 nM，对CDK1/2/5， EGFR， FGFR， PDGFR， InsR等没有抑制活性。Phase 3。 |
| 备注 |
PD0332991 is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 2/3. |
| 生化机理 |
PD 0332991 is a highly selective inhibitor of Cdk4/cyclin D1 and Cdk6/cyclin D2 (IC50’s: Cdk4 = 11 nM; Cdk6 = 16 nM). PD 0332991 has little effect on other protein kinases including EGFR, FGFR, PGFR, and IR. PD 0332991 is a non-ATP competitive inhibitor of Cdk4. PD 0332991 inhibits MDA-MB-435 breast carcinoma cells (IC50 = 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. PD 0332991 shows no activity in Rb-negative cells. PD 0332991 inhibits luminal ER-positive as well as HER2-amplified breast cancer cell lines. PD 0332991 enhances the sensitivity of tamoxifen in the MCF7 tamoxifen-resistant cells. A recent study shows that PD 0332991 could also suppress malignant rhabdoid tumor (MRT) cell lines. |
| 别名 |
6-乙酰基-8-环戊基-5-甲基-2-[[5-(1-哌嗪基)-2-吡啶基]氨基]吡啶并[2,3-d]嘧啶-7(8H)-酮盐酸盐;Palbociclib hydrochloride;Palbociclib HCl; PD-0332991 hydrochloride; PD0332991 hydrochloride; PD 0332991 hydrochloride;6-Acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one hydrochloride;Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-, monohydrochloride |
