|(R)-2-((9-异丙基-6-((4-(吡啶-2-基)苄基)氨基)-9H-嘌呤-2-基)氨基)丁醇|CsnPharm

CAS No.: 294646-77-8

Synonyms: CR8, (R)-Isomer;(R)-CR8;CR8

(R)-CR8 is a cyclin dependent kinase (cdk) inhibitor with IC50 of 0.036 - 0.07 and 0.09 - 0.8 μM for cdk2 and cdk1,respectively.

规格	价格	促销价格	库存	数量

400-920-2911

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生物活性

描述Cyclin-dependent kinases (Cdks) are serine/threonine kinases and their catalytic activities are modulated by interactions with cyclins and Cdk inhibitors (CKIs)^[1]. (R)-CR8 inhibits CDK1/cyclin B (IC50=0. 09 μM), CDK2/cyclin A (0. 072 μM), CDK2/cyclin E (0. 041 μM), CDK5/p25 (0. 11 μM), CDK7/cyclin H (1. 1 μM), CDK9/cyclin T (0. 18 μM) and CK1δ/ε (0. 4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect^[2]. (R)-CR8 (5 mg/Kg; i. p. ) results in a significant reduction in lesion size at 28 days in histological assessment^[3]. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K. The CDK-bound form of (R)-CR8 has a solvent-exposed pyridyl moiety that induces the formation of a complex between CDK12-cyclin K and the CUL4 adaptor protein DDB1, bypassing the requirement for a substrate receptor and presenting cyclin K for ubiquitination and degradation^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01659437	Mycobacterium Ulcerans Infecti... more >>on Collapse <<	Phase 2 Phase 3	Active, not recruiting	January 2018	Benin ... more >> Pobè Treatment Center Pobè, Benin Ghana Agogo Presbyterian Hospital Agogo, Ghana Dunkwa Government Hospital Dunkwa, Ghana Nkawie-Toase Government Hospital Nkawie, Ghana Tepa Government Hosital Tepa, Ghana Collapse <<

实验方案

技术信息

CAS号	294646-77-8	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	C24H29N7O	运输	蓝冰
分子量	431.53	别名	CR8, (R)-Isomer;(R)-CR8;CR8;(R)-Isomer

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