BBO-8520_product_DataBase

Bioactivity	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 [1].
Target	KRASG12C
In Vivo	BBO-8520 (10 mg/kg/d; po) 在 KrasG12C-p53 驱动的 GEMM 模型中引起 pERK 和 KRASG12C 活化抑制，可导致肿瘤持久消退。BBO-8520 还在 KRASG12C 突变肿瘤小鼠中表现出强烈的剂量和时间依赖性药效作用（对 pERK 的抑制超过 80%）[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	2893809-51-1
Formula	C35H33F6N7O2S
Molar Mass	729.74
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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