BBO-10203
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.12%
- CAS No.: 2971769-60-3
- Formula: C34H30F2N6O3S
- Molecular Weight:640.70
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
BBO-10203 (300 nM; 24 h) reduces cell proliferation and pAKT phosphorylation in NCI-H2122<sup>[2]</sup>.
BBO-10203 (24 h) reduces cell proliferation in MCF7<sup>[2]</sup>.
BBO-10203 increases apoptosis in NSCLC<sup>[2]</sup>.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H2122
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Concentration:300 nM
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Incubation Time:24 h
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Result:Led to a significant decrease in cell proliferation and pAKT phosphorylation.
Increased the cleaved caspase-3 positive area, indicating increased apoptosis.
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Cell Line:NCI-H2122
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Concentration:300 nM
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Incubation Time:24 h
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Result:Led to a significant decrease in pAKT phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2971769-60-3
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Appearance Solid
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Molecular Weight 640.70
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Formula C34H30F2N6O3S
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (156.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5608 mL | 7.8040 mL | 15.6079 mL | 39.0198 mL |
| 5 mM | 0.3122 mL | 1.5608 mL | 3.1216 mL | 7.8040 mL | |
| 10 mM | 0.1561 mL | 0.7804 mL | 1.5608 mL | 3.9020 mL | |
| 15 mM | 0.1041 mL | 0.5203 mL | 1.0405 mL | 2.6013 mL | |
| 20 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9510 mL | |
| 25 mM | 0.0624 mL | 0.3122 mL | 0.6243 mL | 1.5608 mL | |
| 30 mM | 0.0520 mL | 0.2601 mL | 0.5203 mL | 1.3007 mL | |
| 40 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 50 mM | 0.0312 mL | 0.1561 mL | 0.3122 mL | 0.7804 mL | |
| 60 mM | 0.0260 mL | 0.1301 mL | 0.2601 mL | 0.6503 mL | |
| 80 mM | 0.0195 mL | 0.0975 mL | 0.1951 mL | 0.4877 mL | |
| 100 mM | 0.0156 mL | 0.0780 mL | 0.1561 mL | 0.3902 mL |
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