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INCB040093

Names

[ CAS No. ]:
1262440-25-4

[ Name ]:
INCB040093

[Synonym ]:
INCB040093
2K59L7G59M
5H-Thiazolo[3,2-a]pyrimidin-5-one, 6-(3-fluorophenyl)-3-methyl-7-[(1S)-1-(9H-purin-6-ylamino)ethyl]-
6-(3-Fluorophenyl)-3-methyl-7-[(1S)-1-(3H-purin-6-ylamino)ethyl]-5H-[1,3]thiazolo[3,2-a]pyrimidin-5-one
UNII:2K59L7G59M
Dezapelisib

Biological Activity

[Description]:

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM; displays 74 to >900-fold selectivity for the other PI3K family members, and does not inhibit a panel of 57 additional kinases; potently inhibits cellular proliferation CD19+ human or CD21+ canine primary B cells with IC50 of 1-3 nM, reduces anti-FcR-induced basophil activation in the presence of human whole blood (IC50=33 nM); demonstrates promising efficacy in patients with Hodgkin's lymphoma in clinical studies. Blood Cancer Phase 2 Clinical

[References]

References 1. Shin N, et al. J Pharmacol Exp Ther. 2017 Nov 10. pii: jpet.117.244947. View Related Products by Target PI3K Blood Cancer

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C20H16FN7OS

[ Molecular Weight ]:
421.451

[ Exact Mass ]:
421.112091

[ LogP ]:
2.57

[ Index of Refraction ]:
1.797

Related Compounds