联系方式：
A-385358产品描述：A-385358 is a selective inhibitor of Bcl-X_L with K_is of 0.80 and 67 nM for Bcl-X_L and Bcl-2, respectively.IC50 & Target: Ki: 0.80 nM (Bcl-X_L), 67 nM (Bcl-2)In Vitro: A-385358 is a selective inhibitor of Bcl-X_L with K_is of 0.80 and 67 nM for Bcl-X_L and Bcl-2, respectively, in fluorescence polarization assays. Treatment of IL-3-deprived FL5.12/Bcl-X_L cells for 24 hours with A-385358 results in cell killing with an EC₅₀ of 0.47±0.05 μM (n=68). This effect is accompanied by an increase in caspase-3 activity. Consistent with the greater affinity for the Bcl-X_L versus Bcl-2 hydrophobic grooves, the EC₅₀ of A-385358 for IL-3-depleted FL5.12/Bcl-2 cells (1.9±0.1 μM; n=55) is 4-fold higher relative to the cytokine-deprived FL5.12/Bcl-X_L cells. In addition, A-385358 is more effective at stimulating cytochrome c release from mitochondria isolated from FL5.12/Bcl-X_L versus Bcl-2 cells^[1].In Vivo: The combination of A-385358 given at 100 mg/kg/d plus the lower dose of paclitaxel produces a significant reduction in tumor growth (%T/C) compare with paclitaxel monotherapy. This combination also yields a >100% increase in time for tumors to reach 900 mm³ (%ILS) compare with vehicle control. Maximal efficacy is observed during the dosing period for A-385358, with slow but steady increase in the tumor growth after termination of treatment. The combination of A-385358 at 75 mg/kg/d plus paclitaxel at 30 mg/kg/d is also well tolerated and inhibits tumor growth rate by nearly 80%. Significant effects on tumor growth relative to paclitaxel monotherapy are observed with doses as low as 50 mg/kg/d^[1].
产品链接：www.medchemexpress.com/A-385358.html

研究领域：Apoptosis

靶点：Bcl-2 Family

相关产品：ABT-199  |  Navitoclax  |  ABT-737  |  S63845  |  A-1210477  |  WEHI-539 hydrochloride  |  A-1155463  |  Obatoclax  |  Bax inhibitor peptide V5  |  A-1331852  |  UMI-77  |  HA14-1  |  BAM7  |  Gambogic Acid  |  Gossypol acetic acid  |  



公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足*新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
大量产品提供免费试用装；已为全球多个知名企业、院校构建各种定制型化合物库。

联系方式：