XL413

广东更新日期：2017-06-12

深圳市浩博世纪生物有限公司

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联系人：谢小姐

电话：0755-29573896拨打

手机：15994704873 拨打

邮箱：2757443387@qq.com

产品详情:

中文名称：: XL413

英文名称：: XL413

CAS号：: 1169558-38-6

XL413的生物活性

XL413 is a potent and selective Cdc7 inhibitor with an IC50 of 3.7 nM, >60-fold selectivity against CK2, >10-fold selectivity against PIM, and >300-fold selectivity against a panel of over 100 protein kinases.
IC50 value: 3.7 nM [1]
Target: Selective Cdc 7
XL413 demonstrated excellent plasma exposures in mice [100 mg/kg (PO): 141 lM (1 h), 81 lM (4 h)]. Prolonged treatment with XL413 (3 days) inhibited the cell proliferation (IC50 = 2685 nM), decreased cell viability (IC50 = 2142 nM) and elicited the caspase 3/7 activity (EC50 = 2288 nM) in Colo-205 cells.XL413 demonstrated an excellent exposure profile infull rat PK assay (dosed at 3 mg/kg: Cmax (PO) = 8.61 lM, AUC(po) = 75 lM h, CL = 117 mL/h kg, Vss = 0.55 L/kg, T1/2 = 2.32 h, F = 95%). Tumor bearing mice were administered XL413 orally at doses of 10, 30, or 100 mg/kg once daily (qd) for 14 days,XL413 was well tolerated at all the doses and regimens examined, with no significant body weight loss observed [1].

化学信息

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分子量

289.72

储存条件

参考CoA中推荐的条件进行储存。

分子式

C14H12ClN3O2

CAS号

1169558-38-6

溶剂/溶解度

10 mM in DMSO

相关文献

[1]. Koltun ES, et al. Discovery of XL413, a potent and selective CDC7 inhibitor. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3727-31.
Abstract
CDC7 is a serine/threonine kinase that has been shown to be required for the initiation and maintenance of DNA replication. Up-regulation of CDC7 is detected in multiple tumor cell lines, with inhibition of CDC7 resulting in cell cycle arrest. In this paper, we disclose the discovery of a potent and selective CDC7 inhibitor, XL413 (14), which was advanced into Phase 1 clinical trials. Starting from advanced lead 3, described in a preceding communication, we optimized the CDC7 potency and selectivity to demonstrate in vitro CDC7 dependent cell cycle arrest and in vivo tumor growth inhibition in a Colo-205 xenograft model.

公司简介

深圳市浩博世纪生物有限公司位于深圳市龙岗区，是一家专业从事科研用生化试剂及相关产品销售的公司；产品涉及生化试剂、化学试剂、抗体、对照标准品、ELISA试剂盒、细胞培养试剂、常用耗材及小仪器等；致力于为生物企业、科研院所、大专院校等提供全方位的科研实验服务。公司与国内外知名企业，科研院校和多家代理商建立了良好的合作关系，是国内产品系列多，品种全，质量优的生物产品和生化试剂供应商。能够满足各生物企业、科研院所、医疗机构的各种需求，能长期提供一站式试剂供应服务。

成立日期	(9年)
注册资本	10万元人民币
员工人数	1-10人
年营业额	￥ 100万以内
经营模式	贸易,试剂,服务
主营行业	化学试剂,通用试剂,格氏试剂,绿色化学产品,基础有机试剂

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