BBO-8520

Catalog No.E1968 Batch:E196801

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Technical Data

Formula

C35H33F6N7O2S

Molecular Weight 729.74 CAS No. 2893809-51-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (137.03 mM)
Ethanol 100 mg/mL (137.03 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description BBO-8520 is a covalent small molecule inhibitor that selectively targets KRAS G12C with high oral bioavailability. It functions as both a KRAS G12C (OFF) inhibitor and a blocker of KRAS G12C (ON) signaling. The compound inhibits cellular proliferation by binding to GTP-bound KRAS G12C (ON), thereby preventing RAS-RAF1 interaction and promoting the transition to the inactive (OFF) state .
In vivo BBO-8520 (10 mg/kg/d; po) causes inhibition of pERK and KRASG12C activation in a KrasG12C-p53-driven GEMM model, leading to durable tumor regression. BBO-8520 demonstrates strong dose-dependent and time-dependent pharmacodynamic effects (more than 80% inhibition of pERK) in mice with KRASG12C mutant tumors.

Protocol (from reference)

References

  • https://aacrjournals.org/cancerres/article/84/7_Supplement/ND07/742758
  • https://link.springer.com/article/10.1007/s40265-023-01980-8

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.