产品说明书
Belvarafenib
 |
同义名 : | HM95573;GDC-5573;RG6185 |
| CAS号 : | 1446113-23-0 | |
| 货号 : | A1158776 | |
| 分子式 : | C23H16ClFN6OS | |
| 纯度 : | 99%+ | |
| 分子量 : | 478.929 | |
| MDL号 : | MFCD31731098 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 12 mg/mL(25.06 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 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] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.44mL 2.09mL 1.04mL |
20.88mL 4.18mL 2.09mL |
| 参考文献 |
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[1]Thieno[3,2-d]pyrimidine derivatives having inhibitory activity for protein kinases |