|(1R)-6-氟-7-(2-氟-6-羟基苯基)-1-[4-甲基-2-(1-甲基乙基)-3-吡啶基]-4-[(S)-2-甲基-4-(1-氧代-2-丙烯-1-基)-1-哌嗪基]-吡啶并[2,3-D]嘧啶-2(1H)-酮|CsnPharm

CAS No.: 2296729-00-3

索托拉西布 Catalog No. CSN24158

Synonyms: AMG-510;AMG-510 racemate;索托拉西布

AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor, which locks KRAS G12C in an inactive GDP-bound state. AMG-510 selectively targets the KRAS p.G12C mutant and shows anti-tumor activity.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

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

描述AMG-510 is a specific covalent inhibitor of K-RAS(G12C) ,which irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. AMG-510 selectively targets the KRAS p.G12C mutant and shows potential antineoplastic activity. KRAS encodes a key signalling protein in tumours, and the G12C KRAS mutation is relatively common in some cancer types. Treatment of KRAS p.G12C lines with covalent KRASG12C inhibitor AMG 510 can increase the expression of HLA^[1].AMG 510 is the first drug candidate to target this mutation^[1]. In clinical trials, AMG 510 demonstrated anti-tumour activity in the first dosing cohorts and represents a potentially transformative therapy for patients^[1].
作用机制AMG-510 selectively forms an irreversible covalent bond to the sulfur atom in the cysteine residue that is present in the mutated form of KRAS, but not in the normal form. KRASG12C can be targeted with covalent small molecule inhibitor AMG-510 which react with the mutant cysteine adjacent to the switch II pocket (SIIP), locking KRAS in its inactive GDP-bound state^[1].
参考文献

[1] Canon J, Rex K, Saiki AY, Mohr C, Cooke K, Bagal D, Gaida K, Holt T, Knutson CG, Koppada N, Lanman BA, Werner J, Rapaport AS, San Miguel T, Ortiz R, Osgood T, Sun JR, Zhu X, McCarter JD, Volak LP, Houk BE, Fakih MG, O'Neil BH, Price TJ, Falchook GS, Desai J, Kuo J, Govindan R, Hong DS, Ouyang W, Henary H, Arvedson T, Cee VJ, Lipford JR. The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity. Nature. 2019 Nov;575(7781):217-223. doi: 10.1038/s41586-019-1694-1. Epub 2019 Oct 30. PMID: 31666701.

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
- 1.7838 mL
- 8.9191 mL
- 17.8382 mL
- 5 mM
- 0.3568 mL
- 1.7838 mL
- 3.5676 mL
- 10 mM
- 0.1784 mL
- 0.8919 mL
- 1.7838 mL

技术信息

CAS号

2296729-00-3

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

C30H30F2N6O3

运输

蓝冰

分子量

560.59

别名

AMG-510;AMG-510 racemate;索托拉西布

溶解度

DMSO	100.0 mg/mL (178.4 mM)
Water	Insoluble
Ethanol	99.0 mg/mL (176.6 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

索托拉西布 Catalog No. CSN24158

靶点选择性

请登录您的专属账户

确认信息