Chemical Structure : PHI-501
CAS No.:
2470433-36-2
PHI-501
(PHI501)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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544.54
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Formula
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C29H23F3N6O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Kim SM, et al. Cancer Cell Int. 2026 Apr 4. doi: 10.1186/s12935-026-04271-w.
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