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BBO-10203 PI3K inhibitor

Cat.No.E5872

BBO-10203 inhibits PI3Kα and KRASG12C by covalently binding to Cys242 in the PI3Kα RAS-Binding Domain. It inhibits both GTP-bound and GDP-bound KRASG12C states, with IC50 and EC50 values of 0.031 nM and 0.02 nM respectively. This compound interferes with RAS-PI3Kα interaction, suppressing RAS-dependent PI3Kα activation. It decreases pERK levels, inhibits cell proliferation, and causes G1 phase arrest and apoptosis. BBO-10203 has potential applications in breast cancer, colorectal cancer, and non-small cell lung cancer research.
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Quality Control

Batch: E587201 DMSO]33 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.90%
99.90

Solubility

In vitro
Batch:

DMSO : 33 mg/mL (51.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 640.70 Formula C34H30F2N6O3S Storage (From the date of receipt)
CAS No. 2971769-60-3 Download SDF Storage of Stock Solutions

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Mechanism of Action

In vivo
BBO-10203 (Oral; once daily) significantly inhibits tumor growth in xenograft models.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-03)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06343402 RECRUITING
Non-small Cell Lung Cancer; Metastatic Non-Small Cell Lung Cancer; NSCLC; KRAS G12C; Metastatic Lung Cancer; Advanced Lung Carcinoma
TheRas, Inc., d/b/a BBOT (BridgeBio Oncology Therapeutics)
2024-05-22 PHASE1
NCT06625775 RECRUITING
Solid Tumor, Adult; Metastatic Breast Cancer; Advanced Breast Cancer; HER2 Mutation-Related Tumors; HER2-positive Metastatic Breast Cancer; KRAS Mutant Metastatic Colorectal Cancer; Metastatic Lung Cancer; Metastatic Colorectal Cancer; Advanced Lung Cancer; HR-positive, HER2-negative Advanced Breast Cancer; HER2-positive Advanced Breast Cancer
TheRas, Inc., d/b/a BBOT (BridgeBio Oncology Therapeutics)
2024-10-29 PHASE1
NCT06917079 RECRUITING
Non-Small Cell Lung Cancer; NSCLC; PDAC - Pancreatic Ductal Adenocarcinoma; CRC (Colorectal Cancer); Metastatic Non-Small Lung Cell Cancer; Metastatic Colorectal Cancer (CRC); KRAS G12A; KRAS G12C; KRAS G12D; KRAS G12S; KRAS G12V; Metastatic Pancreatic Ductal Adenocarcinoma; Advanced Lung Carcinoma; Solid Tumor, Adult
TheRas, Inc., d/b/a BBOT (BridgeBio Oncology Therapeutics)
2025-03-31 PHASE1

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