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MedChemexpress

货号: HY-10087

ABT-263

  • 923564-51-6
  • C47H55ClF3N5O6S3
  • 98%
  • 7日

销 售 价 ¥650.00 /mg

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信息更新时间:2018.06.10
  • ABT-263
  • 98%
  • 5mg
  • 1 mg
  • 7日
  • HY-10087
化合物信息 [查看化合物百科]
化合物英文学名 Navitoclax 化合物中文学名 ABT-263
CAS号 923564-51-6 分子式 C47H55ClF3N5O6S3
分子量 974.613 精确质量 973.296
LogP 11.3995 PSA 170.42
外观与性状 淡黄色固体 折射率 1.654
密度 1.41 g/cm3 熔点 114-116ºC
详细描述
产品描述:ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤1 nM. IC50 Value: ≤ 0.5 nM(Ki for Bcl-xL); ≤1 nM(Ki for Bcl-2); ≤1 nM(Ki for Bcl-w) Target: Bcl-2 Family in vitro: ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263. in vivo: ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. Oral administration of ABT-263 alone causes complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia. In xenograft models of aggressive B-cell lymphoma and multiple myeloma where ABT-263 displays modest or no single agent activity, it significantly enhances the efficacy of clinically relevant therapeutic regimens.
产品链接:http://www.medchemexpress.com/UNC3866.html
产品链接:http://www.medchemexpress.cn/navitoclax.html

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ABT-263

923564-51-6

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