PI3Kα H1047R inhibitor 17

Chemical Structure : PI3Kα H1047R inhibitor 17

Catalog No.: PC-21947Not For Human Use, Lab Use Only.

PI3Kα H1047R inhibitor 17 is a potent, selective H1047R PI3Kα mutant inhibitor with IC50 of 1 nM (inhibition of pAKT formation), without effect on PI3Kα WT.

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Biological Activity

PI3Kα H1047R inhibitor 17 is a potent, selective H1047R PI3Kα mutant inhibitor with IC50 of 1 nM (inhibition of pAKT formation), without effect on PI3Kα WT.
PI3Kα H1047R inhibitor 17 exhibits IC50 of 58 nM in viability assay in T47D (PI3KαH1047R), with low potency against SKBR3 (PI3KαWT) cell lines.
PI3Kα H1047R inhibitor 17 (00 mg/kg, IP, qd) causes tumor regressions in the HCC1954 tumor model in mice.

Physicochemical Properties

M.Wt	364.45
Formula	C22H24N2O3
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	6-Methyl-2-morpholino-8-(1-(phenylamino)ethyl)-4H-chromen-4-one

References

1. Ketcham JM, et al. J Med Chem. 2024 Mar 13. doi: 10.1021/acs.jmedchem.4c00078.

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