PZ0383
帕博昔利
≥98% (HPLC), powder, CDK 4 & 6 inhibitor
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
Product Name
帕博昔利, ≥98% (HPLC)
方案
≥98% (HPLC)
表单
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.）。
制备说明
该化学品可以溶液形式在-80°C保存6个月，-20°C下1个月（避光）。
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
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
ER
Angel L Guerrero-Zotano et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 24(11), 2517-2529 (2018-03-28)
Shinya Kitamura et al.
Cancer science, 113(2), 802-807 (2021-12-07)
Extramammary Paget's disease (EMPD) is a rare adnexal neoplasm commonly seen in the genital areas among the senior population. The prognosis of advanced EMPD is not favorable; thus, the development of potential treatments has long been sought. Cyclin-dependent kinase (CDK)
Flora Doffe et al.
Cancers, 14(15) (2022-07-28)
The recent trend in 3D cell modeling has fostered the emergence of a wide range of models, addressing very distinct goals ranging from the fundamental exploration of cell-cell interactions to preclinical assays for personalized medicine. It is clear that no
David W Fry et al.
Molecular cancer therapeutics, 3(11), 1427-1438 (2004-11-16)
PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4) (IC50, 0.011 micromol/L) and Cdk6 (IC50, 0.016 micromol/L), having no activity against a panel of 36 additional protein kinases. It is a potent antiproliferative agent against retinoblastoma (Rb)-positive
Fiona J Ruiz et al.
Cancers, 13(18) (2021-09-29)
Cervical cancer tumors with undetectable HPV (HPVU) have been underappreciated in clinical decision making. In this study, two independent CC datasets were used to characterize the largest cohort of HPVU tumors to date (HPVU = 35, HPV+ = 430). Genomic
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