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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Raf-PHI-501
PHI-501

Chemical Structure : PHI-501

CAS No.: 2470433-36-2

PHI-501 (PHI501)

货号: PC-26493Not For Human Use, Lab Use Only.

PHI-501 is a potent dual inhibitor of RAF and DDR1/2 with IC50 of 0.30 nM for DDR1 and 8.57 nM for DDR2, inhibits ARAF, BRAF, BRAF V600E, CRAF, and additional BRAF V600 variants (V600A/D/E/K, G464V, and L597V) with IC50 of 1.5-27.8 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PHI-501 is a potent dual inhibitor of RAF and DDR1/2 with IC50 of 0.30 nM for DDR1 and 8.57 nM for DDR2, inhibits ARAF, BRAF, BRAF V600E, CRAF, and additional BRAF V600 variants (V600A/D/E/K, G464V, and L597V) with IC50 of 1.5-27.8 nM.
PHI-501 effectively suppresses the growth of all cell lines, with GI50 values ranging from 0.09262-2.058 uM.
PHI-501 inhibits MAPK signaling in both BRAF- and NRAS-mutant melanoma, dose-dependently inhibits pDDR1, pERK, and pAKT levels in SK-MEL-3 and A375 cells in the presence of collagen.
PHI-501 overcomes resistance to RAF and MEK inhibitors in melanoma cells.
PHI-501 demonstrates in vivo antitumor efficacy in dabrafenib/trametinib–resistant melanoma models.

物理化学性质&存储条件

分子量 544.54
分子式 C29H23F3N6O2
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

Chemical Name/SMILES

N-(4-methyl-3-(7-methyl-2-((6-methylpyridin-3-yl)amino)-8-oxo-7,8-dihydropyrido[3,4-d]pyrimidin-6-yl)phenyl)-3-(trifluoromethyl)benzamide

参考文献

1. Kim SM, et al. Cancer Cell Int. 2026 Apr 4. doi: 10.1186/s12935-026-04271-w.

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