中文名:Obatoclax Mesylate (GX15-070)
英文名:Obatoclax Mesylate (GX15-070)
英文别名:(Z)-2-(5-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-4-methoxy-5H-pyrrol-2-yl)-1H-indole mesylate
纯度:10mM in DMSO
货号:O408971
包装:1ml
Cas号:803712-79-0
存储温度:-80℃储存
产品介绍:
Information
Obatoclax Mesylate (GX15-070) is an antagonist ofBcl-2withKiof 0.22 μM in a cell-free assay, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 3.
In vitro
Obatoclax completely inhibits Bak recovery of Mcl-1 at 5 μM in SK-Mel5 cells and overcomes resistance to ABT-373-induced apoptosis conferred by Mcl-1 in KB/Bcl-2 cells. Obatoclax is a BH3 mimetic which binds to a broad spectrum of Bcl-2 family members, including Bcl-2, Bcl-xL, and Mcl-1. Obatoclax uniquely displaces BH3 domains by activation of the pocket of Mcl-1 followed by a triggering of apoptosis mediated by oligomerization of Bak and release of cytochrome c. Obatoclax is sensitive to Bcl-xL in cell lines lacking it or showing low expression. It shows low cytotoxicity to Mcl-1, Bcl-2, and Bcl-xL in all the strongly-expressed cell lines. Obatoclax inhibits multiple myeloma (MM) cell lines (KMS12PE, KMS18, MY5, etc.) with IC50 values ranging from 52 to 1100 nM and the inhibition is umimpaired even in the presence of IL-6 or IGF-1, which are resistance to cytotoxic agents, at a concentration of 150 nM. Obatoclax enhances the antimyeloma activity induced by melphalan, dexamethasone, or bortezomib. Obatoclax potentiates TRAIL (tumor necrosis factor-related apoptosis-inducing ligand)-mediated apoptosis by unsequestering Bak and Bim from Bcl-2/Bcl-xL or Mcl-1 proteins in PANC-1 and BxPC-3 cells.
In vivo
Obatoclax also exhibits high antitumor activity in SCID mice bearing human C33A cerivical carcinoma tumors at a dose of 0.5 mg/kg.
Cell Data
cell lines:
Concentrations:~10 μM
Incubation Time:48-72 hours
Powder Purity:≥97%
查看阿拉丁官网此产品相关对应页面:https://www.aladdin-e.com/zh_cn/O408971.html
关键字: (Z)-2-(5-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)-4-methoxy-5H-pyrrol-2-yl)-1H-indole mesylate
上海阿拉丁生化科技股份有限公司是A股上市公司((股票代码:688179),专注于科研试剂的研发、生产和销售,已陆续建立多个工厂和研发中心。作为领军企业,阿拉丁始终坚持质量第一,连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种,SKU总数超过46万,产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域,是国内少数化学试剂到生物试剂全面发展的国产试剂品牌,产品同步发布在我们国内外电商平台。