所有图片(1)
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]吡啶基[2,3-d]嘧啶-7（8H）-酮, PD 0332991, PD 332991, PD-0332991, PD0332991, PD991, PF 00080665, PF-00080665, PF00080665, 爱博新
经验公式（希尔记法）:
C24H29N7O2
推荐产品
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
0.1 M HCl: 2 mg/mL, clear
储存温度
room temp
SMILES字符串
CC(C1=C(N2C3CCCC3)N=C(NC4=CC=C(N5CCNCC5)C=N4)N=C1)=C(C(C)=O)C2=O
InChI
1S/C24H29N7O2/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29)
InChI key
AHJRHEGDXFFMBM-UHFFFAOYSA-N
生化/生理作用
PF-00080665（Palbociclib；PD 0332991）是一种靶向周期蛋白依赖性激酶4&6（使用CDK4/cycD3、CDK4/cycD1、CDK6/cycD2的IC50分别为9、11、15 nM；靶向其他36种激酶的IC50为>10 μM）的口服活性且高度特异性的抑制剂，其可有效抑制Cdk4/6依赖性细胞Rb磷酸化过程（IC50 = 66 nM/pSer780 & 63 nM/pSer795； MDA-MB-435）。PF-00080665对Rb阳性的人乳腺癌/结肠癌/肺癌/白血病细胞具有选择性的抗增殖活性（IC50 = 40-400 nM；IC50 >3 μM/Rb阴性MDA-MB-468 & H2009），并且在体内显示出对小鼠多种晚期人类肿瘤异种移植物的有效（12.5-150 mg/kg/day p.o.）。
储存及稳定性
This chemical can be stored in solution at -80°C for 6 months and at -20°C for 1 month (protect from light).
警示用语：
Warning
危险分类
Aquatic Chronic 2 - Muta. 2 - Repr. 2 - STOT RE 2 Oral
靶器官
Bone marrow,male reproductive organs
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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