|6-(二氟甲基)-8-((1R,2R)-2-羟基-2-甲基环戊基)-2-((1-(甲基磺酰基)哌啶-4-基)氨基)吡啶并[2,3-d]嘧啶-7(8H)-酮|CsnPharm

CAS No.: 2185857-97-8

6-(Difluoromethyl)-8-((1R,2R)-2-hydroxy-2-methylcyclopentyl)-2-((1-(methylsulfonyl)piperidin-4-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one Catalog No. CSN24146

Synonyms: PF-3600;Ebvaciclib

PF-06873600 is a selective and orally bioavailable inhibitor of cyclin-dependent kinase (CDK) with Ki of 0.09 nM, 0.13 nM and 0.16 nM for CDK2, CDK4 and CDK6 respectively. PF-06873600 has potential antineoplastic activity.

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技术信息

生物活性

描述Cdks (cyclin-dependent kinases) are the families of protein kinases for regulating the cell cycle. They are involved in regulating transcription, mRNA processing and the differentiation of nerve cells. PF-06873600 is an inhibitor of Cdk2, Cdk4, and Cdk6 (Ki=0.13, 1.25 and 0.11nM, respectively). It is selective for those Cdks over Cdk1 and Cdk9 (Ki= 4.5 and 19.6nM, respectively). PF-06873600 was identified as a candiadate for the treatment of cancer and advanced to phase 1 clinical trail^[1]. In vivo, PF-06873600 (30mg/kg) reduces tumor volume in CTG-0464 and CTG-01912 non small cell lung cancer patient-derived xenograft (PDX) mouse models.
参考文献

[1] Kevin D. Freeman-Cook, Robert L. Hoffman, Douglas C. Behenna, Britton Boras, Jordan Carelli, Wade Diehl, Rose Ann Ferre, You-Ai He, Andrea Hui, Buwen Huang, Nanni Huser, Rhys Jones, Susan E. Kephart, John Lapek, Michele McTigue, Nichol Miller, Brion W. Murray, Asako Nagata, Lisa Nguyen, Sherry Niessen, Sacha Ninkovic, Inish O’Doherty, Martha A. Ornelas, James Solowiej, Scott C. Sutton, Khanh Tran, Elaine Tseng, Ravi Visswanathan, Meirong Xu, Luke Zehnder, Qin Zhang, Cathy Zhang, and Stephen Dann. Journal of Medicinal Chemistry 2021 64 (13), 9056-9077.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1208 mL
- 10.6040 mL
- 21.2079 mL
- 5 mM
- 0.4242 mL
- 2.1208 mL
- 4.2416 mL
- 10 mM
- 0.2121 mL
- 1.0604 mL
- 2.1208 mL

技术信息

CAS号

2185857-97-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H27F2N5O4S

运输

蓝冰

分子量

471.52

别名

PF-3600;Ebvaciclib

溶解度

DMSO	80.0 mg/mL (169.7 mM) warming

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6-(Difluoromethyl)-8-((1R,2R)-2-hydroxy-2-methylcyclopentyl)-2-((1-(methylsulfonyl)piperidin-4-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one Catalog No. CSN24146

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