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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-AM-2383
AM-2383

Chemical Structure : AM-2383

CAS No.: 2791263-84-6

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AM-2383 (AM2383)

货号: PC-27366Not For Human Use, Lab Use Only.

AM-2383 is a potent, selective pan-KRAS inhibitor that blocks signaling via both the GDP(off)- and GTP(on)-bound states of KRAS, potently bind to a diverse set of common oncogenic KRAS mutants with IC50 of 2-10 nM in NanoBRET KRAS target engagement assay, also potently bind to KRAS WT (IC50=2 nM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AM-2383 is a potent, selective pan-KRAS inhibitor that blocks signaling via both the GDP(off)- and GTP(on)-bound states of KRAS, potently bind to a diverse set of common oncogenic KRAS mutants with IC50 of 2-10 nM in NanoBRET KRAS target engagement assay, also potently bind to KRAS WT (IC50=2 nM).
AM-2383 shows little activity toward related RAS isoforms (HRAS Coupled Exchange Activity IC50 = 0.320 (>80-fold selectivity); NRAS Coupled Exchange Activity IC50 = 1.60 μM (>400-fold selectivity).
AM-2383 binds to KRAS WT with a KD value of 0.03 nM, with much weaker affinity for HRAS and NRAS with a KD value of 139 nM and 2.6 uM.
AM-2383 potently inhibits ERK phosphorylation across common KRAS mutants (G12D, G12V, & G12C; IC50 = 3-9 nM) across KRAS mutant cell lines.
AM-2383 showsrobust antiproliferative activity (avg. IC50 = 30 nM) across KRAS mutant cell lines, does not impact proliferation in KRASWT or NRAS mutant cell lines.
AM-2383 (100 mg/kg, QD, oral) induces 80% tumor growth inhibition (TGI) in AsPC-1 tumor xenograft model.

物理化学性质&存储条件

分子量 607.68
分子式 C33H36F3N5O3
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

(R)-1-(7-(8-Ethyl-7-fluoro-3-hydroxynaphthalen-1-yl)-8-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)pyrido[4,3-d]pyrimidin-4-yl)-3-methylpiperidin-3-ol

参考文献

1. Wurz RP, et al. J Med Chem. 2026 Jul 23;69(14):17401-17415.

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