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
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
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Scientific Category
Reference compound1
Clinical Information
Phase 1
Available Sizes
Frequently Asked Questions
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PIP5K2G, CT (Phosphatidylinositol-5-phosphate 4-kinase Type-2 gamma, Phosphatidylinositol-5-phosphate 4-kinase Type II gamma, PI(5)P 4-kinase Type II gamma, PIP4KII-gamma, PIP4K2C, PIP5K2C) (APC)
PIP5K2G, CT (Phosphatidylinositol-5-phosphate 4-kinase Type-2 gamma, Phosphatidylinositol-5-phosphate 4-kinase Type II gamma, PI(5)P 4-kinase Type II gamma, PIP4KII-gamma, PIP4K2C, PIP5K2C) (APC)