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Obatoclax

产品编号 T41278 CAS 803712-67-6

Obatoclax (GX15-070) 是一种 BH3 模拟物，是泛BCL-2家族蛋白抑制剂，对 BCL-2 的Ki 值为 220 nM。Obatoclax 诱导依赖自噬 (autophagy)的细胞死亡，并靶向细胞周期蛋白 D1 进行蛋白酶体降解。Obatoclax 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。

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Obatoclax, CAS 803712-67-6

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

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Obatoclax 的其他形式现货产品:

Obatoclax Mesylate

其他形式的 Obatoclax:

Obatoclax Mesylate
现货

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生物活性

化学信息

存储 & 溶解度

产品描述	Obatoclax (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.
体外活性	Obatoclax (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.
体内活性	Obatoclax (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.

分子量	317.38
分子式	C20H19N3O
CAS No.	803712-67-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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文献引用

1. Zhou X, Qian Y, Ling C, et al.An integrated framework for prognosis prediction and drug response modeling in colorectal liver metastasis drug discovery.Journal of Translational Medicine.2024, 22(1): 321.

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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