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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-BBO-11818
BBO-11818

Chemical Structure : BBO-11818

CAS No.: 3029184-80-0

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BBO-11818 (BBO11818)

货号: PC-26225Not For Human Use, Lab Use Only.

BBO-11818 is a potent, selective, orally bioavailable noncovalent pan-KRAS inhibitor, potently disrupts the interaction of RAF1-RAS Binding Domain (RBD) with KRASG12D (IC50=28 nM), KRASG12V (IC50=61 nM), KRASG12C (IC50=47 nM), and KRASG12R (IC50=51 nM), as well as KRASWT (IC50=120 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BBO-11818 is a potent, selective, orally bioavailable noncovalent pan-KRAS inhibitor, potently disrupts the interaction of RAF1-RAS Binding Domain (RBD) with KRASG12D (IC50=28 nM), KRASG12V (IC50=61 nM), KRASG12C (IC50=47 nM), and KRASG12R (IC50=51 nM), as well as KRASWT (IC50=120 nM).
BBO-11818 inhibits multiple KRAS mutants in both the inactive GDP-bound (OFF) and active GTP-bound (ON) states.
BBO-11818 potently inhibits SOS-mediated nucleotide exchange of KRAS WT and oncogenic mutants but not NRAS WT.
BBO-11818 is highly potent in multiple KRAS-mutant cells, including those with KRASG12D, KRASG12V, and KRASG12C, with pERK inhibition EC50 values ranging from 0.356 to 28.1 nM, also potently inhibits pERKin a cell line harboring KRASAMP with EC50 of 4.35 nM.
BBO-11818 does not inhibit pERK in cell lines not driven by KRAS.
BBO-11818 also showed limited potency in the KRASG12R and KRASQ61X lines tested (EC50 = 357 and 278 nmol/L, respectively.
BBO-11818 inhibits cellular viability in cells harboring the clinically important mutants KRASG12D, KRASG12V, and KRASG12C, with mean EC50 values of 2.21, 31.2, and 2.26 nmol/L, respectively.
BBO-11818 produced tumor regressions in KRAS-mutant xenograft models, strongly reduced tumor pERK and DUSP6 levels in a dose- and time-dependent manner.

物理化学性质&存储条件

分子量 733.73
分子式 C34H33F6N7O3S
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

methyl (3S)-3-((7-(2-amino-3-cyano-7-fluorobenzo[b]thiophen-4-yl)-8-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-6-(trifluoromethyl)quinazolin-4-yl)(ethyl)amino)pyrrolidine-1-carboxylate

参考文献

1. Stahlhut C, et al. Cancer Discov. 2026 Mar 6:OF1-OF20.

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