|4-氨基-N-(1-((3-氯-2-氟苯基)氨基)-6-甲基异喹啉-5-基)噻吩并[3,2-d]嘧啶-7-甲酰胺|CsnPharm

CAS No.: 1446113-23-0

Belvarafenib Catalog No. CSN24269

Synonyms: HM95573;GDC-5573;RG6185

Belvarafenib is a pan-RAF inhibitor, with IC50 values of 56 nM, 7 nM and 5 nM for B-RAF, B-RAF^V600E and C-RAF, respectively.

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技术信息

生物活性

描述Among the various cytoplasmic kinases, RAF (Rapidly Accelerated Fibrosarcoma) is one of the kinases that participate in the linear Ras-RAF-MEK-ERK mitogen-activated protein kinase (MAPK) pathway initiated by a receptor protein kinase, which is activated by a growth factor^[1]. Belvarafenib, currently in Phase 1 clinical trials, is a selective and orally bioavailable pan-RAF kinase inhibitor. When biochemically assayed for hundreds of kinases, Belvarafenib showed selectivity toward RAF family kinases, including strong inhibition activities for BRAF WT, BRAF mutants and CRAF. Belvarafenib strongly inhibits the growth of cancer cell lines with BRAF, NRAS or KRAS mutations and also shows excellent anticancer efficacy in animal models using the corresponding cancer cells. The phosphorylation of ERK, AKT and S6K are inhibited after the treatment of Belvarafenib in the above cancer cells of BRAF, NRAS or KRAS mutations^[2]. Belvarafenib was well tolerated and exhibited anti-tumor activity in patients with advanced solid tumors harboring RAS or RAF mutations^[3]
参考文献

[1] Thieno[3,2-d]pyrimidine derivatives having inhibitory activity for protein kinases
[2] Identification of signal transduction kinases inhibited by pan-RAF inhibitor belvarafenib using FRET imaging technique
[3] Belvarafenib, a novel pan-RAF inhibitor, in solid tumor patients harboring BRAF, KRAS, or NRAS mutations: Phase I study

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
- 2.0880 mL
- 10.4400 mL
- 20.8799 mL
- 5 mM
- 0.4176 mL
- 2.0880 mL
- 4.1760 mL
- 10 mM
- 0.2088 mL
- 1.0440 mL
- 2.0880 mL

技术信息

CAS号

1446113-23-0

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H16ClFN6OS

运输

蓝冰

分子量

478.93

别名

HM95573;GDC-5573;RG6185

溶解度

DMSO	11.47 mg/mL (24.0 mM)
Water	insoluble

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