PI3Kβ and δ inhibitor 20a ( —— )

Catalog No. M12847 CAS No. 1842380-77-1

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Product Name

PI3Kβ and δ inhibitor 20a
Note

Research use only, not for human use.
Brief Description

A potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively.
Description

A potent, highly selective PI3Kβ/δ inhibitor with IC50 of 7.8/5.3 nM respectively, with liitle to no activity on PI3Kα/γ (IC50=850/>10,000 nM); inhibits the phosphorylation of AKT1 Ser473 in PI3K-dependent cell lines with EC50 of 3.4-7.3 nM, inhibits AKT Ser473 phosphorylation and cell viability of LNCaP tumor cells with EC50 of 7.3 nM and GI50 of 38 nM; demonstrates efficacy in human PTEN-deficient LNCaP prostate carcinoma xenograft tumor model.
Synonyms

——
Pathway

PI3K/Akt/mTOR signaling
Target

PI3K
Recptor

PI3K
Research Area

——
Indication

——

CAS Number

1842380-77-1
Formula Weight

450.26
Molecular Formula

C17H14Cl2FN9O
Purity

>98% (HPLC)
Solubility

——
SMILES

FC1=CC(Cl)=C(N=C([C@@H](NC2=C(Cl)C(N)=NC(N)=N2)C)N(C3=NNC=C3)C4=O)C4=C1
Chemical Name

(S)-8-chloro-2-(1-((2,6-diamino-5-chloropyrimidin-4-yl)amino)ethyl)-6-fluoro-3-(1H-pyrazol-3-yl)quinazolin-4(3H)-one

1. Perreault S, et al. J Med Chem. 2017 Feb 23;60(4):1555-1567.

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