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Chemical Structure : BBO-8956
Catalog No.: PC-21686Not For Human Use, Lab Use Only.
BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.
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BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.
BBO-8956 selectively binds to KRAS G12C in SW2/α3 pocket, in both active (GTP) and inactive (GDP)-bound conformation.
BBO-8956 effectively binds GTP-KRAS G12C, shifts the state 1 - state 2 equilibrium to an inactive "sub-state" representing state 1-like conformation, and disrupts the effector binding and downstream oncogenic signaling.
BBO-8956 potently disrupts KRAS G12C/RAF1(RBD) interaction with an IC50 of 57 nM in KRAS G12C-GppNHp and 411 nM in KRAS G12C-GTP.
BBO-8956 inhibits ERK phosphorylation in KRAS G12C-mutant cell lines, lung adenocarcinoma NCI-H358 and pancreatic ductal adenocarcinoma MiaPaCa-2.
| M.Wt | 711.76 | |
| Formula | C35H34F5N7O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Alok K Sharma, et al. J Biol Chem. 2024 Jan 16:105650.
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