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BBO-10203
🥰Excellent
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
🥰Excellent
Purity: 98.62%
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 | |
| 5 mg | $4,120 | - | 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:98.62%
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Color | White |
| Appearance | Solid |
Storage & Solubility Information
| 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: 80 mg/mL (124.86 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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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 mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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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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