2. PI3K/Akt/mTOR MAPK/ERK Pathway GPCR/G Protein
  3. PI3K Ras Akt
  4. 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.

For research use only. We do not sell to patients.

BBO-10203

BBO-10203 Chemical Structure

CAS No. : 2971769-60-3

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Based on 1 publication(s) in Google Scholar

BBO-10203 Related Antibodies

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  • Purity & Documentation

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Description

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].

In Vitro

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.

BBO-10203 Related Antibodies

Cell Proliferation Assay[2]

Cell Line: NCI-H2122
Concentration: 300 nM
Incubation Time: 24 h
Result: Led to a significant decrease in cell proliferation and pAKT phosphorylation.
Increased the cleaved caspase-3 positive area, indicating increased apoptosis.

Western Blot Analysis[2]

Cell Line: NCI-H2122
Concentration: 300 nM
Incubation Time: 24 h
Result: Led to a significant decrease in pAKT phosphorylation. 
In Vivo

BBO-10203 (Oral; once daily) significantly inhibits tumor growth in xenograft models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

640.70

Formula

C34H30F2N6O3S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5608 mL 7.8040 mL 15.6079 mL
5 mM 0.3122 mL 1.5608 mL 3.1216 mL
View the 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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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BBO-10203 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BBO-102032971769-60-3BBO10203BBO 10203PI3KRasAktPhosphoinositide 3-kinasePKBProtein kinase BRAS-PI3Kα signaling pathway,apoptosis,G1 arrestInhibitorinhibitorinhibit

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