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BBO-8520

目录号 : GC73788

BBO-8520是一种直接靶向KRAS G12C的小分子共价抑制剂,具有很高的口服可用性。

BBO-8520 Chemical Structure

Cas No.:2893809-51-1

规格 价格 库存 购买数量
1 mg
¥5,220.00
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Sample solution is provided at 25 µL, 10mM.

Description

BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state .

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[1].

References:
[1]. Maciag A E, et al. Abstract ND07: BBO-8520, a first-in-class, direct inhibitor of KRASG12C (ON), locks GTP-bound KRASG12C in the state 1 conformation resulting in rapid and complete blockade of effector binding[J]. Cancer Research, 2024, 84(7_Supplement): ND07-ND07. [2]. Caughey B A, Strickler J H. Targeting KRAS-Mutated Gastrointestinal Malignancies with Small-Molecule Inhibitors: A New Generation of Breakthrough Therapies[J]. Drugs, 2024, 84(1): 27-44.

化学性质

Cas No. 2893809-51-1 SDF
分子式 C35H33F6N7O2S 分子量 729.74
溶解度 DMSO : ≥ 50 mg/mL (68.52 mM) 储存条件 4°C, protect from light, stored under nitrogen
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.3704 mL 6.8518 mL 13.7035 mL
5 mM 0.2741 mL 1.3704 mL 2.7407 mL
10 mM 0.137 mL 0.6852 mL 1.3704 mL
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