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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-SHY-855
SHY-855

Chemical Structure : SHY-855

CAS No.: 2446485-15-8

SHY-855 (SHY855)

货号: PC-25520Not For Human Use, Lab Use Only.

SHY-855 (SHY855) is a potent, non-covalent small molecule inhibitor of pan-Ras superfamily, competes with GTP binding to K-Ras WT, the G12D, G12C and Q61H mutants, as well as Rac-1 and Rho-A, with IC50 values of 2.5-5 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SHY-855 (SHY855) is a potent, non-covalent small molecule inhibitor of pan-Ras superfamily, competes with GTP binding to K-Ras WT, the G12D, G12C and Q61H mutants, as well as Rac-1 and Rho-A, with IC50 values of 2.5-5 uM.
SHY-855 robustly inhibits GTP binding to the K-Ras variants.
SHY-855 inhibits phosphorylation and activation of MEK, Erk1/2 and Akt in PANC-1, MIA PaCa-2 and NCI-H1975 cell lines with IC50 of 1-3 uM.
SHY-855 prevent Ras-GTP complex formation with IC50 of 2-3 uM in PANC-1, MIA PaCa-2 and NCI-H1975 cells in Ras pull-down assays.
SHY-855 bind directly to the GTP-binding site of Ras.
SHY-855 inhibits cellular proliferation with IC50 of 0.45-1.2 uM in PANC-1, MIA PaCa-2, NCI-H1975), BxPC3 (K-Ras WT) and A549 (K-Ras G12S mutant) and NCI-H1299 (N-Ras Q61K mutant).

物理化学性质&存储条件

分子量 506.02
分子式 C26H24ClN5O2S
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

6-(2-chloro-3-methoxyphenyl)-N-(2-methoxyethyl)-2-(1-methyl-1H-imidazol-2-yl)-5-phenylthieno[2,3-d]pyrimidin-4-amine

参考文献

1. Luca Carta, et al. Mol Cancer Ther. 2025 Sep 12:OF1-OF10.

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