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XL413

基本信息 产品图片 产品描述 供应商联系方式 同类产品

基本信息:

  • 发布时间: 2017-06-12
  • 产品名称: XL413
  • 产品英文名称: XL413
  • CAS号: 1169558-38-6
  • 产品包装: 10mg
  • 产品价格: 1860元/罐
  • 有效期: 一年

产品图片:

XL413

产品描述:

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

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.

  • 供应商联系方式:
  • 联系人 谢小姐
  • 公司名称 深圳市浩博世纪生物有限公司
  • 电话 0755-29573896
  • 手机 15994704873
  • 传真 
  • 邮箱 2757443387@qq.com
  • 地址 龙岗区布吉街道荣华路中加名园14号楼1号201