Chemical Structure : SHY-867
CAS No.:
2446484-96-2
SHY-867
(SHY867)
Catalog No.: PC-25521Not For Human Use, Lab Use Only.
SHY-867 (SHY867) 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 1.25-5.0 uM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
SHY-867 (SHY867) 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 1.25-5.0 uM.
SHY-867 robustly inhibits GTP binding to the K-Ras variants.
SHY-867 inhibits phosphorylation and activation of MEK, Erk1/2 MIA PaCa-2 and NCI-H1975 cell lines with IC50 of 1 uM, of Akt, wiht IC50 of 7 µM in PANC-1 and MIA PaCa-2 and 10 µM in NCI-H1975
SHY-867 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-867 bind directly to the GTP-binding site of Ras.
SHY-867 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).
Physicochemical Properties
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M.Wt
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485.61
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Formula
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C26H27N7OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Thieno[2,3-d]pyrimidin-4-amine, N-[(1R,3S)-3-methoxycyclopentyl]-2-(1-methyl-1H-imidazol-2-yl)-6-(1-methyl-1H-pyrazol-3-yl)-5-phenyl-, rel-
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References
1. Luca Carta, et al. Mol Cancer Ther. 2025 Sep 12:OF1-OF10.
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