产品资料

XL888---HSP90Inhibitor

如果您对该产品感兴趣的话,可以
产品名称: XL888---HSP90Inhibitor
产品型号: M60164-5s
产品展商: 其它品牌
产品文档: 无相关文档

简单介绍

XL888---HSP90Inhibitor


XL888---HSP90Inhibitor  的详细介绍
Product Information
Molecular Weight: 503.64
Formula: C29H37N5O3
Purity: ≥98%
CAS#: 1149705-71-4
Solubility: DMSO up to 100 mM
Chemical Name: 5-((R)-sec-butylamino)-N1-((1R,3s,5S)-8-(5-(cyclopropanecarbonyl)pyridin-2-yl)-8-azabicyclo[3.2.1]octan-3-yl)-2-methylterephthalamide
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

XL888 is a highly potent, ATP-competitive and orally bioavailable small-molecule inhibitor of heat shock protein 90 (Hsp90) with antineoplastic activity. It specifically binds to Hsp90 with an IC50 of 24 nM. XL888 inhibits HSP90’s chaperone function and promotes the proteasomal degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival. In vivo XL888 significantly induces the regression of, or growth inhibition of established M229R and 1205LuR xenografts in SCID mice. XL888 treatment is noted to be proapoptotic in vivo and leads to increased TUNEL staining in M229R xenografts associated with increased expression of BIM and decreased expression of Mcl-1. 

 

How to Use:

  • In vitro: XL888 was used at 10 µM in vitro and in cellular assays.
  • In vivo: XL888 was orally dosed to mice at 100 mg/kg 3 times a week in xenograft models

 

Reference: 

  1. 1. Haarberg HE, et al. Inhibition of Wee1, AKT, and CDK4 underlies the efficacy of the HSP90 inhibitor XL888 in an in vivo model of NRAS-mutant melanoma. (2013) Mol Cancer Ther. 12(6):901-12.
  2. 2. Bussenius J, et al. Discovery of XL888: a novel tropane-derived small molecule inhibitor of HSP90. (2012) Bioorg Med Chem Lett. 22(17):5396-404.
  3. 3. Paraiso KH, et al. The HSP90 inhibitor XL888 overcomes BRAF inhibitor resistance mediated through diverse mechanisms.(2012) Clin Cancer Res. 18(9):2502-14.
  4. 4. Lyman SK, et al. High-content, high-throughput analysis of cell cycle perturbations induced by the HSP90 inhibitor XL888. (2011) PLoS One. 6(3):e17692. 

 


     

Products are for research use only. Not for human use.

产品留言
标题
联系人
联系电话
内容
验证码
点击换一张
注:1.可以使用快捷键Alt+S或Ctrl+Enter发送信息!
2.如有必要,请您留下您的详细联系方式!

沪公网安备 31011202007337号