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PI3Kβ and δ inhibitor 20a

Chemical Structure : PI3Kβ and δ inhibitor 20a

CAS No.: 1842380-77-1

PI3Kβ and δ inhibitor 20a

Catalog No.: PC-61135Not For Human Use, Lab Use Only.

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).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

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.

Physicochemical Properties

M.Wt 450.259
Formula C17H14Cl2FN9O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(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

References

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

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