|(R)-6,7-二甲氧基-2-甲基-N-(1-(4-(2-((甲基氨基)甲基)苯基)噻吩-2-基)乙基)喹唑啉-4-胺|CsnPharm

CAS No.: 2244904-70-7

BAY-293 Catalog No. CSN24479

Synonyms: (R)-6,7-Dimethoxy-2-methyl-N-(1-(4-(2-((methylamino)methyl)phenyl)thiophen-2-yl)ethyl)quinazolin-4-amine

BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21nM.

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400-920-2911

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技术信息

生物活性

描述Mutations in the RAS genes have been recognized as major oncogenes with a high occurrence rate in human cancers. RAS proteins act as molecular switches that cycle between an active, GTP-bound state and an inactive, GDP-bound state. Activated by guanine nucleotide exchange factors (GEFs), RAS in its GTP bound state interacts with a number of effectors. The most-studied GEF for RAS is the protein Son of Sevenless (SOS) for which two human isoforms, SOS1 and SOS2, are known^[1]. BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC₅₀ of 21 nM. BAY-293 is a potent inhibitor of SOS1^[1]. BAY-293 (595 nM-3580 nM; 72h) shows efficient antiproliferative activity against wild-type KRAS cell lines (K-562, MOLM-13) and cell lines with KRAS^G12C mutation (NCI-H358, Calu-1). BAY-293 efficiently inhibited pERK (extracellular signal-regulated kinase) levels in K-562 cells after incubation for 60 min without affecting total protein levels of ERK^[1].
作用机制The side-chain amino group of BAY-293 forms two new hydrogen bonds, to Asp887 and Tyr884, and is in a favorable position for a cation–π interaction with the side chain of Tyr884.
参考文献

[1] Hillig RC, Sautier B, Schroeder J, Moosmayer D, Hilpmann A, Stegmann CM, Werbeck ND, Briem H, Boemer U, Weiske J, Badock V, Mastouri J, Petersen K, Siemeister G, Kahmann JD, Wegener D, Böhnke N, Eis K, Graham K, Wortmann L, von Nussbaum F, Bader B. Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction. Proc Natl Acad Sci U S A. 2019 Feb 12;116(7):2551-2560. doi: 10.1073/pnas.1812963116. Epub 2019 Jan 25. PMID: 30683722; PMCID: PMC6377443.

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
- 2.2293 mL
- 11.1463 mL
- 22.2925 mL
- 5 mM
- 0.4459 mL
- 2.2293 mL
- 4.4585 mL
- 10 mM
- 0.2229 mL
- 1.1146 mL
- 2.2293 mL

技术信息

CAS号

2244904-70-7

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C25H28N4O2S

运输

蓝冰

分子量

448.58

别名

(R)-6,7-Dimethoxy-2-methyl-N-(1-(4-(2-((methylamino)methyl)phenyl)thiophen-2-yl)ethyl)quinazolin-4-amine

溶解度

DMSO	90.0 mg/mL (200.6 mM)
Water	Insoluble
Ethanol	90.0 mg/mL (200.6 mM)

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