文献支持Obatoclax Mesylate (GX15-070 Mesylate) 是 BH3 模拟物,是泛 BCL-2 家族蛋白抑制剂
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保存条件 :4℃
保质期 :详见说明
英文名 :Obatoclax Mesylate
库存 :充足
供应商 :杭州昊鑫生物
CAS号 :803712-79-0
规格 :2mg
Obatoclax Mesylate (Synonyms: 奥巴克拉甲磺酸盐 ; GX15-070 Mesylate)
Obatoclax Mesylate (GX15-070 Mesylate) 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 Mesylate 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 Mesylate 具有抗癌和广谱抗寄生虫 (antiparasitic) 活性。美国medchemexpress(MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商,总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物,拥有着多年的发展历程和丰富的行业经验。从产品的HNMR数据解析到生物活性数据,从客户的询价到产品的售后服务,我们拥有着完善的管理体系,从而保证我们的服务更加高效、准确。努力为中国的医药行业发展注入新的活力,我们将成为您研发工作值得信赖的伙伴。
生物活性
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity[3][4].
体外研究(In Vitro)
Obatoclax Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM[2].
Obatoclax Mesylate (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[1].
Obatoclax Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells[3].
Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations[1].
Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM[1].
Obatoclax Mesylate 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 Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells[1].
Obatoclax Mesylate (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.
体内研究
(In Vivo)
Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits 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
413.49
性状
Solid
Formula
C21H23N3O4S
CAS 号
803712-79-0
中文名称
奥巴克拉甲磺酸盐
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶解性数据
In Vitro:
DMSO : 12.5 mg/mL (30.23 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.4184 mL 12.0922 mL 24.1844 mL
5 mM 0.4837 mL 2.4184 mL 4.8369 mL
10 mM 0.2418 mL 1.2092 mL 2.4184 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
1.
请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution
2.
请依序添加每种溶剂: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.83 mg/mL (2.01 mM); Clear solution
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