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Association details:
| Biomarker: | NRAS mutation |
|---|---|
| Cancer: | Melanoma |
| Drug: | PHI-501 (pan-RAF inhibitor, DDR inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
411 / 6 - PHI-501, a novel pan-RAF/DDRs dual kinase inhibitor, overcomes BRAF or MEK inhibitor resistance in melanoma
Published date:
03/15/2023
Excerpt:
PHI-501 demonstrated potent growth inhibition (GI50 <1 µM) in seven melanoma cell lines harboring BRAF V600E or NRAS mutations….PHI-501 triggered apoptosis more effectively than these inhibitors...PHI-501 had 74-fold more inhibitory effect on cell proliferation (GI50: 0.55 µM to 40 µM). Moreover, treatment with PHI-501 strongly suppressed cell migration of cobimetinib-resistant SK-MEL-30 cells....Melanoma cells resistant to RAF or MEK-targeted treatments or harboring NRAS mutation exhibited strong antiproliferative activity when treated with PHI-501.
