Pemigatinib Chemical Properties

Boiling point:

697.6±55.0 °C(Predicted)

Density 

1.44±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO:40.0(Max Conc. mg/mL);82.05(Max Conc. mM)

form 

A crystalline solid

pka

11.56±0.40(Predicted)

color 

White to light yellow

Pemigatinib Usage And Synthesis

Binding Mode

Pemigatinib binds to the inactive conformation of FGFR1 with the activation loop adopting a DFG-in conformation (type I1/2 inhibitor). The pyrrolopyridine moiety forms two hydrogen bonds with the NH and the carbonyl of Ala564 in the hinge region (Figs. 3, 4). The difluoromethoxyphenyl ring, which is perpendicular relative to the tricyclic ring, fits the specificity pocket containing the gatekeeper residue Val561. One of the methoxy oxygen atoms hydrogen bonds to the backbone NH of Asp641. The terminal morpholine extends towards the solventfront region, and makes only minor contacts with the protein.

Uses

Pemigatinib is a potent inhibitor of FGFRs for the treatment of cholangiocarcinoma.

Indications

Pemigatinib is indicated for the treatment of previously treated adult patients with unresectable locally advanced or metastatic cholangiocarcinoma (CCA) who have been identified by an FDA-approved test for the presence of fibroblast growth factor receptor 2 (FGFR2) fusions or other rearrangements.

brand name

Pemazyre

General Description

Class: receptor tyrosine kinase; Treatment: metastatic cholangiocarcinoma; Other name: INCB054828; Elimination half-life = 15 h; Protein binding = 90.6%

target

Primary targets: Pan-FGFR

IC 50

FGFR1/2/3/4 IC 50 = 0.4, 0.5, 1, 30 nM