BBO-10203

BBO-10203 is a potent inhibitor of PI3Kα and KRASG12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRASG12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer[1][2].

Product Specifications

CAS Number

[2971769-60-3]

UNSPSC

12352005

Target

Akt; PI3K

Type

Reference compound

Related Pathways

PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bbo-10203.html

Purity

99.12

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CN(N=C1)C(C=C2)=C1C=C2C3=NC(C4=NN5C([C@@H](C)N(C(C=C)=O)CC5)=C4)=[C@]([C@]6=C(F)C=C(F)C=C6OCCOC)C7=C3C=CS7

Molecular Formula

C34H30F2N6O3S

Molecular Weight

640.70

References & Citations

[1]Fan Z, et al. Precise regulation of RAS-Mediated PI3Kα activation: therapeutic potential of BBO-10203 in cancer treatment. Exp Hematol Oncol. 2025;14 (1) :115. Published 2025 Sep 29.|[2]Kerstin W. Sinkevicius, et al. Abstract C082: BBO-10203, a first-in-class, orally bioavailable, selective breaker of the RAS:PI3Kα interaction inhibits tumor growth alone and in combination with KRAS inhibitors in KRAS mutant models without inducing hyperglycemia. Mol Cancer Ther (2025) 24 (10_Supplement) : C082.