INCB040093 ( INCB 040093;INCB-040093;Dezapelisib )

Catalog No. M11094 CAS No. 1262440-25-4

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Product Name

INCB040093
Note

Research use only, not for human use.
Brief Description

A novel potent, selective, orally available PI3Kδ inhibitor with IC50 of 31 nM.
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
Synonyms

INCB 040093;INCB-040093;Dezapelisib
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

PI3K
Research Area

Cancer
Indication

Blood cancer

CAS Number

1262440-25-4
Formula Weight

421.45
Molecular Formula

C20H16FN7OS
Purity

>98% (HPLC)
Solubility

——
SMILES

O=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4N=CNC4=NC=N3)C)N=C5N1C(C)=CS5
Chemical Name

6-(3-fluorophenyl)-3-methyl-7-((1S)-1-(9H-purin-6-ylamino)ethyl)-5H-(1,3)thiazolo(3,2-a)pyrimidin-5-one

1. Shin N, et al. J Pharmacol Exp Ther. 2017 Nov 10. pii: jpet.117.244947.

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