2893809-52-2
Chemical Structure
(4R)-BBO-8520
- CAS No.: 2893809-52-2
- Formula:C35H33F6N7O2S
- Molecular Weight:729.74
InChIKey: RIVFEDYNLHJKEZ-VHJOERAISA-N
SMILES: FC1=[C@@](C(C(F)(F)F)=CC2=C(N=C(N=C21)OC[C@@]34CCCN3C[C@@H](C4)F)N5[C@H](CN([C@@H](C5)C)C(C=C)=O)C)[C@@]6=CC=C(F)C7=C6C(C#N)=C(N)S7
Biological Activity: (4R)-BBO-8520 (Compound 314), an isomer of BBO-8520 (HY-158107), 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 KRASG12C (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].
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(4R)-BBO-8520 | (4R)-BBO-8520 (Compound 314), an isomer of BBO-8520 (HY-158107), 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 KRASG12C (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. | |||||||||||||||||||||
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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.
