Obatoclax B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Obatoclax (GX15-070) 是 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 诱导自噬 (autophagy) 依赖性细胞死亡，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。

Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.

Obatoclax (GX15-070) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM. 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 IC50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively. Obatoclax (400 nM; for 24 hours) induces autophagy in OSCC cells. Obatoclax (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations.Obatoclax (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM.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. Obatoclax (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells. Cell Proliferation Assay 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 Cell Line:AW8507 and SCC029B cells Concentration:400 nM Incubation Time:24 hours Result:Induced autophagy in OSCC cells.Cell Cycle Analysis 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 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.

Obatoclax (GX15-070; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner. Animal Model:6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors 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.

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803712-67-6

317.38

C20H19N3O

>98% (HPLC)

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C(=C1N=C(C=C1OC)C2=CC=3C(N2)=CC=CC3)C4=C(C)C=C(C)N4

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(-20℃)

With Ice Pack

≥ 2 years