中文名：CCT245737
英文名：CCT245737
纯度：Moligand™，≥99%
货号：C413955
Cas号：1489389-18-5
存储温度：-20°C储存
运输条件：超低温运输
产品介绍：
Information
CCT245737 (SRA737, PNT-737) is an orally activeCHK1inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1.
Targets
Chk1 (Cell-free assay) 1.4 nM
In vitro
CCT245737 is a potent inhibitor of recombinant human CHK1 with IC50 of 1.4±0.3 nM (mean±SD, n = 3, EZ Reader II assay). There is > 1,000-fold selectivity for CHK1 versus the functionally important kinases CDK1 and CHK2 (IC50=1.26-2.44 and 9.03 μM, respectively), and at least a 90-fold selectivity against cross-reacting kinases such as ERK8, PKD1, RSK1 and 2. CCT245737 potently inhibits cellular CHK1 activity (IC50 30-220nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It can abrogate an etoposide-induced G2/M arrest. CCT245737 has high cell permeability, as measured by transport across a CaCo2 cell monolayer.
In vivo
Mouse oral bioavailability is complete (100%) with extensive tumor exposure. CCT245737 shows significant single-agent activity against a MYC-driven mouse model of B-cell lymphoma. An i.v. dose of 10mg/kg CCT245737 into BALB/c mice gives a peak plasma concentration of 4μmol/L, with a half-life of 2.86h, an AUC0-∞ of 9.96μmol.h/L, a plasma clearance of 2.1L/h/kg and a large volume of distribution (0.19L). The equivalent oral dose gave an almost identical profile with an AUC0-∞ of 10.4μmol.h/L showing complete oral bioavailability (F = 105%). In a word, CCT245737 shows complete oral bioavailability with linear pharmacokinetics and high tumor/plasma ratios consistent with extensive tumor exposure. Adequate CCT245737 tumor drug exposure takes a significant antitumor activity.
Cell Research(from reference)
Cell lines：The colon tumor cell lines HT29 and SW620, the pancreatic cancer cell line MiaPaCa-2 and the non-small cell lung cancer Calu6 cell line
Incubation Time：96 h
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/C413955.html
关键字： (R)-5-((4-((morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile ; (R)5-((4-((Morpholin-2-ylmethyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)pyrazine-2-carbonitrile ; 2-Pyrazinecarbonitrile, 5-((4-(((2R)-2-morpholin
阿拉丁（A股科创板上市企业，股票代码：688179） 是科研服务领域的领先供应商与制造商，拥有科学服务领域领导品牌：阿拉丁。核心业务涵盖高端化学与生化试剂、生命科学、小分子及化合物库及材料科学四大领域，并自主拥有“芯硅谷”实验耗材品牌，依托电商平台实现线上主导的销售模式 。产品广泛服务于985/211高校、科研院所及生物医药、化工材料等领域220余家A股上市公司。
国内以上海化工园区、奉贤基地为核心，建成超7.6万㎡现代化产业集群 ，拥有GMP车间满足高品质多元需求，并配备全国五大仓储中心。研发投入超3亿元，建有化学、生物两大研发中心，每年推出超10,000种新产品，截至2025年10月拥有178项知识产权 ，产品SCI引用超25.3万篇，稳居国内科研试剂文献TOP3 。
战略立足全球，已在美国、德国等多地设5个公司布局 ，连续获《国家级专精特新“小巨人”企业》 、《中国化学试剂十强企业》 、《最受用户欢迎试剂品牌》 等荣誉，秉承“推动发现，推进科学”的理念，助力科研创新。