BBO-8956 | KRAS G12C inhibitor | Probechem Biochemicals

Chemical Structure : BBO-8956

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BBO-8956 (BBO8956, BBO 8956)

货号: 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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1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	711.76
分子式	C35H34F5N7O2S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Alok K Sharma, et al. J Biol Chem. 2024 Jan 16:105650.

BBO-8956 (BBO8956, BBO 8956)

生物&药学活性

物理化学性质&存储条件

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询单

BBO-8956 (BBO8956, BBO 8956)

生物&药学活性

物理化学性质&存储条件

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