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BBO-8520
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Catalog No. T85809Cas No. 2893809-51-1
Alias BBO8520
BBO-8520 is a first-in-class, direct dual inhibitor of both the active (ON) and inactive (OFF) conformational states of KRASG12C. BBO-8520 binds to the Switch-II/Helix3 pocket of KRASG12C, covalently modifying the target cysteine residue and thereby disabling effector binding in the ON state. BBO-8520 exhibits potent inhibition of KRAS signaling under growth factor-activated conditions, where existing OFF-only inhibitors demonstrate minimal activity. In vivo, BBO-8520 rapidly engages its target and suppresses signaling, resulting in durable tumor regression across multiple models, including those resistant to OFF-only KRASG12C inhibitors.
BBO-8520
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Purity: 97.87%
Catalog No. T85809Alias BBO8520Cas No. 2893809-51-1
BBO-8520 is a first-in-class, direct dual inhibitor of both the active (ON) and inactive (OFF) conformational states of KRASG12C. BBO-8520 binds to the Switch-II/Helix3 pocket of KRASG12C, covalently modifying the target cysteine residue and thereby disabling effector binding in the ON state. BBO-8520 exhibits potent inhibition of KRAS signaling under growth factor-activated conditions, where existing OFF-only inhibitors demonstrate minimal activity. In vivo, BBO-8520 rapidly engages its target and suppresses signaling, resulting in durable tumor regression across multiple models, including those resistant to OFF-only KRASG12C inhibitors.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $396 | - | In Stock | |
| 5 mg | $716 | - | In Stock | |
| 10 mg | $993 | - | In Stock | |
| 25 mg | $1,590 | - | In Stock | |
| 50 mg | $2,430 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $1,150 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:97.87%
Appearance:Solid
Color:White
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | BBO-8520 is a first-in-class, direct dual inhibitor of both the active (ON) and inactive (OFF) conformational states of KRASG12C. BBO-8520 binds to the Switch-II/Helix3 pocket of KRASG12C, covalently modifying the target cysteine residue and thereby disabling effector binding in the ON state. BBO-8520 exhibits potent inhibition of KRAS signaling under growth factor-activated conditions, where existing OFF-only inhibitors demonstrate minimal activity. In vivo, BBO-8520 rapidly engages its target and suppresses signaling, resulting in durable tumor regression across multiple models, including those resistant to OFF-only KRASG12C inhibitors. |
| In vivo | BBO-8520 (10 mg/kg/d; po) inhibits pERK and KRAS G12C activation in the KrasG12C-p53 driven GEMM model, resulting in sustained tumor regression. Additionally, BBO-8520 demonstrates a strong dose- and time-dependent pharmacodynamic effect in KRASG12C mutant tumor-bearing mice, with pERK inhibition exceeding 80% [1]. |
| Synonyms | BBO8520 |
| Molecular Weight | 729.74 |
| Formula | C35H33F6N7O2S |
| Cas No. | 2893809-51-1 |
| Smiles | N#CC1=C(SC2=C(F)C=CC(=C12)C=3C(F)=C4N=C(N=C(C4=CC3C(F)(F)F)N5CC(N(C(=O)C=C)CC5C)C)OCC67N(CCC6)CC(F)C7)N |
| Storage | keep away from direct sunlight,store under nitrogen,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO: ≥ 40 mg/mL, Sonication is recommended. |
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.74 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. |
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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
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
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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