PHI-501

PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma[1].

Product Specifications

CAS Number

2470433-36-2

UNSPSC

12352005

Target

Discoidin Domain Receptor; Interleukin Related; JAK; MEK; Raf; Ras; STAT; TNF Receptor

Related Pathways

Apoptosis; Epigenetics; GPCR/G Protein; Immunology/Inflammation; JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Field of Research

Cancer

Smiles

O=C(C1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C)C(C3=CC4=C(C(N3C)=O)N=C(NC5=CN=C(C)C=C5)N=C4)=C2

Molecular Formula

C29H23F3N6O2

Molecular Weight

544.53

References & Citations

[1]Kim SM, et al. PHI-501 is a novel potent next-generation pan-RAF/DDRs inhibitor, and overcomes resistance to RAF or MEK inhibitor in melanoma via dual inhibition of RAF and DDR1/2 signaling. Cancer Research. 2024 Mar 22;84 (6_Supplement) :4657-.