Catalog No.: PC-24644Not For Human Use, Lab Use Only.
BBO-10203 is a first-in-class inhibitor of the RAS-PI3Kα interaction, binds specifically and cocalently to the RBD of PI3Kα (IC50=3 nM), disrupts PI3Kα interaction with K-,H-, and N-RAS with low single digit nanomolar potency (5 nM).
BBO-10203 is a first-in-class inhibitor of the RAS-PI3Kα interaction, binds specifically and cocalently to the RBD of PI3Kα (IC50=3 nM), disrupts PI3Kα interaction with K-,H-, and N-RAS with low single digit nanomolar potency (5 nM).
BBO-10203 does not inhibit the kinase activity of PI3Kα, forms covalent bond with C242.
blocks binding of K-, H-, and N-RAS to PI3Kα.
BBO-10203 potently inhibits pAKT with single digit nM potency (IC50=4 nM), inhibits basal pAKT cellular levels (BT-474/KYSE-410 IC50: ~5 nM) in HER2 amplified (HER2amp) and wild-type or mutant PI3Ka cell lines.
BBO-1020 (1-100 mg/kg, PO) induces dependent inhibition of pAKT in KYSE-410 (HER2amp/KRASG12C) tumor bearing mice.
BBO-10203 daily oral dosing of 30 mg/kg results in significant tumor regressions in KYSE-410 xenograft model.
BBO-10203 inhibits pAKT leading to monotherapy and combination benefit with KRASi in KRAS mutant tumors.
