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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-XMU-MP-9
XMU-MP-9

Chemical Structure : XMU-MP-9

CAS No.: 2251130-41-1

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XMU-MP-9

货号: PC-26395Not For Human Use, Lab Use Only.

XMU-MP-9 is bifunctional, specific small molecule K-RAS mutants degrader, facilitates NEDD4-1-mediated ubiquitination and degradation of various oncogenic K-RAS mutants.

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50 mg ￥1280 In stock
100 mg ￥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

XMU-MP-9 is bifunctional, specific small molecule K-RAS mutants degrader, facilitates NEDD4-1-mediated ubiquitination and degradation of various oncogenic K-RAS mutants.
XMU-MP-9 could induce decrease of endogenous K-RASG12V protein levels in SW620 cells as early as 12 h treatment and reached a maximum effect at 36 to 48 h.
XMU-MP-9 exhibits potent effect on inhibiting growth of NEDD4-1+/+ SW620 cells in 2-D culture and 3-D soft agar in comparison to NEDD4-1−/− SW620 cells, also induces NEDD4-1-dependent decrease of endogenous K-RASG12V protein levels.
XMU-MP-9 primarily assists NEDD4-1 in attaching ubiquitin to K128 of K-RASG12V.
XMU-MP-9 interacted with both K-RASG12V and NEDD4-1 with similar binding affinities (Kd = 18.4 and 25.4 nM).
XMU-MP-9 promotes ubiquitination and degradation of various K-RAS mutants such as G12D, G12C, G12S, G13V, G13D, and Q61H via lysosomal pathway, but not H-RAS or N-RAS mutants.
XMU-MP-9 inhibits proliferation and anchorage-independent growth of K-RAS mutant harboring cancer cells.
XMU-MP-9 (40 mg/kg once or twice daily via tail vein injection) suppresses tumor development of K-RAS mutant harboring cancer cells in vivo.

物理化学性质&存储条件

分子量 385.84
分子式 C19H13ClFN3OS
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

N-(2-Chloro-6-fluorobenzyl)-5-(1H-indazol-3-yl)thiophene-3-carboxamide

参考文献

1. Taoling Zeng, et al. Acta Pharm Sin B. 2026 Feb;16(2):979-993.

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