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BBO-8520
🥰Excellent
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
🥰Excellent
Purity: 97.879%
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $424 | In Stock | |
| 5 mg | $1,060 | In Stock | |
| 10 mg | $1,700 | In Stock | |
| 25 mg | $3,400 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $1,700 | In Stock |
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Purity:97.879%
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Color | White |
| Appearance | Solid |
Storage & Solubility Information
| 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. |
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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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