(4R)-BBO-8520 (Compound 314), an isomer of BBO-8520, is a selective KRAS G12C inhibitor. 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. (4R)-BBO-8520 can be used for the research of cancer [1] [2] [3].
References:
[1]. Bin Wang, et al. Compositions and methods for inhibition of ras. WO2023004102A2. 2024-01-23
[2]. 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.
[3]. 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.
References:
[1]. Bin Wang, et al. Compositions and methods for inhibition of ras. WO2023004102A2. 2024-01-23
[2]. 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.
[3]. 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.