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
产品名称
帕博昔利, ≥98% (HPLC)
SMILES string
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
0.1 M HCl: 2 mg/mL, clear
storage temp.
room temp
Preparation Note
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）。
Biochem/physiol Actions
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.）。
signalword
Warning
hcodes
Hazard Classifications
Aquatic Chronic 2 - Muta. 2 - Repr. 2 - STOT RE 2 Oral
target_organs
Bone marrow,male reproductive organs
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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)
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)
Max Heckler et al.
Cancer discovery, 11(10), 2564-2581 (2021-05-05)
CDK4/6 inhibitors are approved to treat breast cancer and are in trials for other malignancies. We examined CDK4/6 inhibition in mouse and human CD8+ T cells during early stages of activation. Mice receiving tumor-specific CD8+ T cells treated with CDK4/6
The anti-tumor efficacy of CDK4/6 inhibition is enhanced by the combination with PI3K/AKT/mTOR inhibitors through impairment of glucose metabolism in TNBC cells.
Daniele Cretella et al.
Journal of experimental & clinical cancer research : CR, 37(1), 72-72 (2018-03-29)
我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.
联系客户支持