BBO-8520 | KRAS G12C inhibitor | Probechem Biochemicals

Chemical Structure : BBO-8520

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BBO-8520 (BBO8529, BBO 8520)

货号: PC-22123Not For Human Use, Lab Use Only.

BBO-8520 is a potent, selective and covalent inhibitor of KRAS G12C (ON), locks GTP-bound KRASG12C in the state 1 conformation resulting in rapid and complete blockade of effector binding.

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生物&药学活性

BBO-8520 is a potent, selective and covalent inhibitor of KRAS G12C (ON), locks GTP-bound KRASG12C in the state 1 conformation resulting in rapid and complete blockade of effector binding.
BBO-8520 binds in the switch II pocket and covalently modifies both the (ON) and (OFF) forms of KRASG12C independently of any other partner proteins.
BBO-8520 inhibits KRASG12C (ON) by locking the GTP-bound protein in state 1.
BBO-8520 displays highly significant binding to KRAS G12C in a global cysteine proteome analysis and is 100x more selective for KRASG12C than for WT KRAS and other mutant isoforms, with no measurable activity against N- or H-RAS.
BBO-8520 has sub-nanomolar potency against KRASG12C mutant cell lines.
BBO-8520 rapidly and completely blocks the RAS-RAF1 interaction in effector binding assays, at least 30x more potent than sotorasib and adagrasib at preventing outgrowt in long-term clonogenic assays.
BBO-8520 (10 mg/kg, daily dosing, oral) causes significant tumor volume regression in the KrasG12C-p53 driven GEMM model, exhibits in vivo target engagement and pERK inhibition in the MIAPaCa-2 and H358 KRASG12C mutant tumor models.

物理化学性质&存储条件

分子量	729.75
分子式	C35H33F6N7O2S
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-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-6-(trifluoromethyl)quinazolin-7-yl)-2-amino-7-fluorobenzo[b]thiophene-3-carbonitrile

参考文献

1. Anna E. Maciag, et al. Cancer Res (2024) 84 (7_Supplement): ND07.

BBO-8520 (BBO8529, BBO 8520)

生物&药学活性

物理化学性质&存储条件

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BBO-8520 (BBO8529, BBO 8520)

生物&药学活性

物理化学性质&存储条件

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