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PI3Kα-IN-5

Chemical Structure : PI3Kα-IN-5

CAS No.: 2101744-13-0

PI3Kα-IN-5

Catalog No.: PC-62838Not For Human Use, Lab Use Only.

PI3Kα-IN-5 is a potent, selective PI3Kα inhibitor with enzyme IC50 and cell IC50 of 6 nM and 87 nM respectively, exhibits 100-fold selectivity over PI3Kβ.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PI3Kα-IN-5 is a potent, selective PI3Kα inhibitor with enzyme IC50 and cell IC50 of 6 nM and 87 nM respectively, exhibits 100-fold selectivity over PI3Kβ; displays high potency and selectivity, and suitable physiochemical and pharmacokinetic properties for oral administration; shows good inhibition of tumour growth (86% tumour growth inhibition at 50 mg/kg twice daily orally) in the MCF7 xenograft model in mice.

Physicochemical Properties

M.Wt 363.385
Formula C17H17N9O
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

5-(3-amino-6-(imidazo[1,2-a]pyridin-3-yl)-5-methylpyrazin-2-yl)-N,1-dimethyl-1H-1,2,4-triazole-3-carboxamide

References

1. Barlaam B, et al. Bioorg Med Chem Lett. 2017 Jul 1;27(13):3030-3035.

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