|rel-(αR,4R)-2-氨基-6-溴-4-(1-氰基-2-乙氧基-2-甲酰)-4H-苯并呋喃-3-羧酸|CsnPharm

CAS No.: 65673-63-4

rel-(R)-Ethyl 2-amino-6-bromo-4-((R)-1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate(relative) Catalog No. CSN11133

Synonyms: HA14-1

HA14-1 inhibits Bcl-2 with IC50 of ~9 μM by binding to the surface pocket and disturb the interaction of Bax/Bcl-2, it's cell-permeable.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Bcl-2

IC50:9μM
描述Bcl-2 (B-cell lymphoma 2) is an integral outer mitochondrial membrane protein that regulates cell death by inhibiting Bax, thus controlling the mitochondrial membrane permeability. Bcl-2 could engage a group of proapoptotic Bcl-2 family members, the BH3-only proteins like Bid and Bim, by physically sequestering them from directly activating Bax. Bcl-2 could also interact with Bax directly^[3]. HA14-1 is an inhibitor of Bcl-2. In a binding assay, HA14-1 was found to bind the designated pocket on Bcl-2 with the IC50 of ≈ 9 μM in competing with the bcl-2 binding of Flu-BakBH3^[4]. In a MTT assay, the lethal concentration 50% (LC50) values of HA14-1 to HF1A3, HF4.9 and HF28RA cells when incubated for 20h were 4.5 μM, 12.6 μM and 8.1 μM, respectively^[5]. Treatment with 50 μM HA14-1 by 3h induced apoptosis in HL-60 cells as evidenced by DNA ladders^[4]. In a BeGBM xenograft model established in nude mice, HA14-1 was injected once weekly for 4 weeks at the concentration of 400 nM in 100 μl volume at the site of cell injection. This dose of HA14-1 increased the effect of etoposide on tumor growth^[3].
作用机制HA14-1 is an inhibitor of Bcl-2. In a binding assay, HA14-1 was found to bind the designated pocket on Bcl-2 with the IC50 of ≈ 9 μM in competing with the bcl-2 binding of Flu-BakBH3^[4].
动物研究
剂量
Rabbit: 2 mg/kg^[3] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rabbit: 2 mg/kg^[3] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4436 mL
- 12.2180 mL
- 24.4361 mL
- 5 mM
- 0.4887 mL
- 2.4436 mL
- 4.8872 mL
- 10 mM
- 0.2444 mL
- 1.2218 mL
- 2.4436 mL

技术信息

CAS号

65673-63-4

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H17BrN2O5

运输

蓝冰

分子量

409.23

别名

HA14-1

溶解度

DMSO	82.0 mg/mL (200.4 mM)
Water	Insoluble
Ethanol	82.0 mg/mL (200.4 mM)

动物实验配方

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rel-(R)-Ethyl 2-amino-6-bromo-4-((R)-1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate(relative) Catalog No. CSN11133

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