Chemical Structure : BBO-8956
CAS No.:
2892617-27-3
BBO-8956
(BBO8956, 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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711.76
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Formula
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C35H34F5N7O2S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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4-(4-((2S,5R)-4-acryloyl-2,5-dimethylpiperazin-1-yl)-8-fluoro-2-((tetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-6-(trifluoromethyl)quinazolin-7-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile
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References
1. Alok K Sharma, et al. J Biol Chem. 2024 Jan 16:105650.
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