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  • 化合物 Obatoclax|T41278|TargetMol

化合物 Obatoclax|T41278|TargetMol

Obatoclax
803712-67-6
17500 100mg 起订
13800 50mg 起订
10600 25mg 起订
上海 更新日期:2024-12-12

TargetMol中国(陶术生物)

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联系人:邵小姐
手机:4008200310 拨打
邮箱:marketing@tsbiochem.com

产品详情:

中文名称:
化合物 Obatoclax
英文名称:
Obatoclax
CAS号:
803712-67-6
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
99.44%
产品类别:
抑制剂
货号:
T41278

Product Introduction

Bioactivity

NameObatoclax
DescriptionObatoclax (GX15-070), a pan-BCL-2 family proteins inhibitor and BH3 mimetic, exhibits a binding affinity (K_i) of 220 nM for BCL-2. It promotes autophagy-dependent cell death and cyclin D1 degradation via the proteasome. Additionally, Obatoclax demonstrates anti-cancer properties and broad-spectrum antiparasitic activity.
In vitroObatoclax (GX15-070) shows inhibition of BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM [2]. Obatoclax (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC 50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively [1]. Obatoclax (400 nM; for 24 hours) induces autophagy in OSCC cells [3]. Obatoclax (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations [1]. Obatoclax (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM [1]. Obatoclax induces T286 phosphorylation-dependent or -independent cyclin D1 degradation. in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax inhibits GSK3β but activates p38 MAPK, while barely affecting ERK1/2 activity in HT-29 cells [1]. Obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells [1]. Cell Proliferation Assay [1] Cell Line: human colorectal cancer HCT116, HT-29 and LoVo cells Concentration: 50, 100, 200 nM Incubation Time: 24, 48, and 72 hours Result: Induced a dose- and time-dependent reduction of cell numbers. Cell Autophagy Assay [3] Cell Line: AW8507 and SCC029B cells Concentration: 400 nM Incubation Time: 24 hours Result: Induced autophagy in OSCC cells. Cell Cycle Analysis [1] Cell Line: HCT116 and HT-29 cells Concentration: 50, 100, 200 nM Incubation Time: 24 hours Result: Provoked a dose-dependent increase in the G1-phase cell populations. Western Blot Analysis [1] Cell Line: HCT116, HT-29 and LoVo cells Concentration: 50, 100, 200 nM Incubation Time: 24 hours Result: Indicated a marked drop in cyclin D1 levels as low as 50 nM.
In vivoObatoclax (GX15-070; 1.15-5 mg/kg; intravenously injected; five consecutive days) shows potent antitumor activity in xenograft mouse models in a dose-dependent manner [4]. Animal Model: 6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors [4] Dosage: 1.15, 2.5, 5 mg/kg Administration: Intravenously injected (through lateral tail vein); five consecutive days (i.e. 5 injections) Result: Exhibited potent antitumor activity in xenograft mouse models in a dose-dependent manner.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
KeywordsObatoclax
Obatoclax|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 566.265100万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务

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