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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-LUNA18
LUNA18

Chemical Structure : LUNA18

CAS No.: 2676177-63-0

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LUNA18 (LUNA-18)

货号: PC-22631Not For Human Use, Lab Use Only.

LUNA18 (LUNA-18) is a highly potent, 11-mer cyclic peptide inhibitor for the intracellular tough target RAS with IC50 of <2 nM for KRAS G12D-SOS1 PPI, KD of 0.043 nM for KRAS G12C.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LUNA18 (LUNA-18) is a highly potent, 11-mer cyclic peptide inhibitor of KRAS with IC50 of <2 nM for KRAS G12D-SOS1 PPI, KD of 0.043 nM for KRAS G12C.
LUNA18 has a cellular IC50 of 1.4 nM in AsPC-1 viability assay.
LUNA18 showed significant cellular efficacy (IC50 = 0.17-2.9 nM) against cell lines with KRAS genetic alterations, such as LS180 (colon cancer, KRASG12D), GSU (stomach cancer, KRASG12D), NCI-H441 (non-small cell lung cancer (NSCLC), KRASG12V), NCI-H2122 (NSCLC, KRASG12C), and MiaPaCa-2 (pancreatic cancer, KRASG12C), in addition to AsPC-1.
LUNA18 (10 mg/kg, oral, once daily for 14 days) exhibits in vivo tumor growth inhibition in in mice bearing an NCI-H441 (KRAS G12V) or a MiaPaCa-2 (KRASG12C) xenograft.

物理化学性质&存储条件

分子量 1437.71
分子式 C73H105F5N12O12
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

(5S,8S,11S,15S,18S,23aS,29S,35S,37aS)-8-((S)-sec-butyl)-18-cyclopentyl-29-(3,5-difluoro-4-(trifluoromethyl)phenethyl)-36-ethyl-11-isobutyl-N,N,5,6,12,16,19,33-octamethyl-35-(4-methylbenzyl)-4,7,10,13,17,20,23,28,31,34,37-undecaoxotetratriacontahydro-2H,4H-spiro[azeto[2,1-u]pyrrolo[2,1-i][1,4,7,10,13,16,19,22,25,28,31]undecaazacyclotetratriacontine-21,1'-cyclopentane]-15-carboxamide

参考文献

1. Tanada M, et al. J Am Chem Soc. 2023 Aug 2;145(30):16610-16620.

2. Nomura K, et al. J Med Chem. 2022 Oct 13;65(19):13401-13412.

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