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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-PF-07284890
PF-07284890

Chemical Structure : PF-07284890

CAS No.: 2573781-75-4

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PF-07284890 (Tinlorafenib, ARRY-461, ARRY461, PF 07284890)

货号: PC-72612Not For Human Use, Lab Use Only.

Tinlorafenib (PF-07284890, ARRY-461) is an orally bioavailable, brain penetrant, potent, small molecule BRAF V600 mutants inhibitor, inhibits BRAF and CRAF with IC50 of 5.8 and 4.1 nM, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tinlorafenib (PF-07284890, ARRY-461) is an orally bioavailable, brain penetrant, potent, small molecule BRAF V600 mutants inhibitor, inhibits BRAF and CRAF with IC50 of 5.8 and 4.1 nM, respectively.
PF-07284890 inhibits the clinically relevant kinase domain BRAF V600 mutants (V600E and V600K) with IC50 of 24-25 nM.
PF-07284890 potently inhibits phosphorylation of ERK, a downstream marker of BRAF inhibition, and potently inhibits proliferation of BRAF V600E/K mutant melanoma cell lines (IC50=18-38 nM).
PF-07284890 inhibits phosphorylation of ERK in A375 BRAF V600E tumors, achieving maximal target inhibitions at a dose of 10 mg/kg.
PF-07284890 (10-30 mg/kg BID) caused significant and durable tumor regressions in the intracranial A375-luc BRAF V600E melanoma xenograft model.

物理化学性质&存储条件

分子量 456.89
分子式 C19H19ClF2N4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO (4.6 mg/mL)
Chemical Name/SMILES

N-[2-Chloro-3-[(3,4-dihydro-3,5-dimethyl-4-oxo-6-quinazolinyl)amino]-4-fluorophenyl]-3-fluoro-1-propanesulfonamide

参考文献

1. Patent WO2020261156A1.

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