1262440-25-4

1262440-25-4 structure

Name: INCB040093
Chemical Name: Dezapelisib
CAS Number: 1262440-25-4
Molecular Formula: C₂₀H₁₆FN₇OS
Molecular Weight: 421.451
Create Date: 2020-01-11 12:13:59
Modify Date: 2024-04-06 20:13:06
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

Name	Dezapelisib
Synonyms	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

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