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BBO-10203
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Catalog No. T203428Cas No. 2971769-60-3
Alias BBO10203
BBO-10203 is an orally active small molecule, also designated as Compound 758, that functions as a selective PI3Kα-Ras interaction disruptor by binding to the Ras-binding domain of PI3Kα. BBO-10203 effectively prevents Ras-PI3Kα complex formation, inhibits downstream Akt activation without altering basal PI3Kα kinase activity, thereby minimizing risks of hyperglycemia and hyperinsulinemia, and displays selective antitumor activity against KRAS-mutant malignancies, making it an important investigational candidate for targeted cancer therapeutics.
BBO-10203
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Purity: 99.87%
Catalog No. T203428Alias BBO10203Cas No. 2971769-60-3
BBO-10203 is an orally active small molecule, also designated as Compound 758, that functions as a selective PI3Kα-Ras interaction disruptor by binding to the Ras-binding domain of PI3Kα. BBO-10203 effectively prevents Ras-PI3Kα complex formation, inhibits downstream Akt activation without altering basal PI3Kα kinase activity, thereby minimizing risks of hyperglycemia and hyperinsulinemia, and displays selective antitumor activity against KRAS-mutant malignancies, making it an important investigational candidate for targeted cancer therapeutics.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $1,980 | In Stock | In Stock | |
| 5 mg | $4,120 | In Stock | In Stock | |
| 10 mg | $5,630 | - | In Stock | |
| 25 mg | $8,460 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.87%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | BBO-10203 is an orally active small molecule, also designated as Compound 758, that functions as a selective PI3Kα-Ras interaction disruptor by binding to the Ras-binding domain of PI3Kα. BBO-10203 effectively prevents Ras-PI3Kα complex formation, inhibits downstream Akt activation without altering basal PI3Kα kinase activity, thereby minimizing risks of hyperglycemia and hyperinsulinemia, and displays selective antitumor activity against KRAS-mutant malignancies, making it an important investigational candidate for targeted cancer therapeutics. |
| In vitro | BBO-10203 blocks the interaction between KRAS-G12D and PI3Kα in HEK293T cells with an IC50 of 6 nM, without affecting the binding between KRAS-G12D and protein kinase CRAF or inhibiting the in vitro kinase activity of PI3Kα. BBO-10203 exhibits an IC50 < 10 nM against most HER2 gene-amplified cell lines and is sensitive to PIK3CA spiral mutations in cell lines. [1][2] |
| In vivo | In fasting male mice undergoing an oral glucose tolerance test, 300 mg/kg BBO-10203 did not affect glucose metabolism, while 50 mg/kg aprelis was associated with hyperglycaemia and hyperinsulinaemia.
In xenograft mouse models with KRAS G12X mutations, with or without PIK3CA mutations, BBO-10203 (10–100 mg/kg, oral, once daily, for 28 days) exhibited dose-dependent tumour volume reduction effects and antitumour efficacy in several subcutaneous xenograft models with multiple KRAS mutations. [1] |
| Synonyms | BBO10203 |
| Molecular Weight | 640.7 |
| Formula | C34H30F2N6O3S |
| Cas No. | 2971769-60-3 |
| Smiles | O=C(C=C)N1CCN2N=C(C=C2C1C)C=3N=C(C=4C=CC5=C(C=NN5C)C4)C=6C=CSC6C3C7=C(F)C=C(F)C=C7OCCOC |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (390.2 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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