pemigatinib-hcl

Description: Pemigatinib HCl (formerly INCB-054828) is a potent, orally bioavailable and selective FGFR inhibitor with IC50 values of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has potential antineoplastic activity for treatment of cholangiocarcinoma. INCB054828 binds to and inhibits FGFR1/2/3, which may result in the inhibition of FGFR1/2/3-related signal transduction pathways. This inhibits proliferation in FGFR1/2/3-overexpressing tumor cells.

References:

1. ArudraK, et al. Calcinosis cutis dermatologic toxicity associated withfibroblast growth factor receptor inhibitor for the treatment of Wilmstumor. J Cutan Pathol. 2018 Oct; 45(10):786-790.

2. RoskoskiR Jr, et al. The role of fibroblast growth factor receptor (FGFR)protein-tyrosine kinase inhibitors in the treatment of cancers includingthose of the urinary bladder. Pharmacol Res. 2020 Jan; 151:104567.

3. KrookMA, et al. Tumor heterogeneity and acquired drug resistance inFGFR2-fusion-positive cholangiocarcinoma through rapid research autopsy.Cold Spring Harb Mol Case Stud. 2019 Aug 1; 5(4).

Related CAS #:1513857-77-6 (free base)