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产品名称
帕博昔利, ≥98% (HPLC)
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
0.1 M HCl: 2 mg/mL, clear
儲存溫度
room temp
SMILES 字串
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 密鑰
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.)。
儲存和穩定性
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)。
訊號詞
Warning
危險分類
Aquatic Chronic 2 - Muta. 2 - Repr. 2 - STOT RE 2 Oral
標靶器官
Bone marrow,male reproductive organs
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
其他客户在看
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)
E Martínez de Dueñas et al.
Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico (2018-03-23)
Cyclin-dependent kinases (CDKs) play a key role in cell cycle regulation, which makes them a clear therapeutic target to interfere with cell division and proliferation in cancer patients. Palbociclib, a specific inhibitor of CDK4/6 with outstanding clinical efficacy data and
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)
Abeer J Al-Qasem et al.
NPJ precision oncology, 6(1), 68-68 (2022-09-25)
Resistance to aromatase inhibitor (AI) treatment and combined CDK4/6 inhibitor (CDK4/6i) and endocrine therapy (ET) are crucial clinical challenges in treating estrogen receptor-positive (ER+) breast cancer. Understanding the resistance mechanisms and identifying reliable predictive biomarkers and novel treatment combinations to
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
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