CAS:630124-46-8AST-487

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AST-487 Cat No. FB06221Cas No. 630124-46-8

Synonyms: NVP-AST 487

AST-487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.

规格	价格	促销价格	库存

18817579266

立即询价

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18817579266

立即询价

实验数据

储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8884 mL
- 9.4418 mL
- 18.8837 mL
- 5 mM
- 0.3777 mL
- 1.8884 mL
- 3.7767 mL
- 10 mM
- 0.1888 mL
- 0.9442 mL
- 1.8884 mL
计算器摩尔计算器总药量计算器工作液计算器

技术信息

CAS号

630124-46-8

储存条件

粉末: -20°C 3 年

液体: -80°C 12 月

分子式

C26H30F3N7O2

运输

蓝冰

分子量

529.56

别名

NVP-AST 487

溶解度

DMSO	130.0 mg/mL (245.5 mM)
Water	insoluble

动物实验配方

靶点数据

生物活性

描述The RET kinase has emerged as a promising target for the therapy of medullary thyroid cancers (MTC) and of a subset of papillary thyroid cancers. AST-487, a N, N′-diphenyl urea with an IC₅₀ of 0.88 μM on RET kinase, inhibited RET autophosphorylation and activation of downstream effectors, and potently inhibited the growth of human thyroid cancer cell lines with activating mutations of RET but not of lines without RET mutations. AST-487 induced a dose-dependent growth inhibition of xenografts of NIH3T3 cells expressing oncogenic RET, and of the MTC cell line TT in nude mice. Additionally, AST-487 inhibited calcitonin gene expression in vitro in TT cells, in part, through decreased gene transcription. After a single oral administration of 15 mg/kg of AST-487 to OF1 mice, a mean peak plasma level (C_max) of 0.505±0.078 μM SE is achieved after 0.5 h. Similar levels of AST 487 are found in the plasma of mice up to 6 h after oral administration, with a C_last of 21±4 nM at 24 h.