应用 |
PD 0332991 isethionate has been used:
· to incubate MCF10A cells to verify cyclin D1 inhibition of autophagy involved cyclin-dependent kinase activity
· as a cyclin dependent kinase 4 (CDK4) inhibitor to study its anticonvulsive property in Drosophila
· to mimic the inhibitory effect of 5α-dihydrotestosterone (DHT) on HPr-1AR cell cycle progression and growth |
产品介绍 |
Palbociclib (PD0332991) Isethionate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。 |
合法信息 |
Sold for only research purposes |
备注 |
Palbociclib (PD0332991) Isethionate 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 potent selective inhibitor of cyclin dependent kinases CDK4 and CDK6 with in vitro IC50 = 11 nM (CDK4) and 16 nM (CDK6). PD 0332991 induces G1 arrest in retinoblastoma (Rb)-positive tumor cells. PD 0332991 might act as a chemsensitizer. It is useful in the treatment of breast cancer along with antioestrogens. PD 0332991 is also known to possess antitumor action. |
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2-羟基 - 乙磺酸(1:1), 帕博西尼羟乙基磺酸盐;PD0332991 isethionate; PD-0332991 isethionate; PD 0332991 isethionate;6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one 2-hydroxy-ethanesulfonic acid (1:1) |