|1-(4-((4-乙基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)-3-(4-((6-(甲基氨基)嘧啶-4-基)氧基)苯基)脲|CsnPharm

CAS No.: 630124-46-8

AST 487 Catalog No. CSN18365

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. AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM.

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技术信息

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^[3]. 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^[3]. 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^[3].
参考文献

[1] Weisberg E, Roesel J, et al. Antileukemic effects of the novel, mutant FLT3 inhibitor NVP-AST487: effects on PKC412-sensitive and -resistant FLT3-expressing cells. Blood. 2008 Dec 15;112(13):5161-70.
[2] Akeno-Stuart N, Croyle M, et al. The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64.
[3] Akeno-Stuart N, Croyle M, Knauf JA, Malaguarnera R, Vitagliano D, Santoro M, Stephan C, Grosios K, Wartmann M, Cozens R, Caravatti G, Fabbro D, Lane HA, Fagin JA. The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64. doi: 10.1158/0008-5472.CAN-06-4605. PMID: 17638907.

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
- 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

技术信息

CAS号

630124-46-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -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

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