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SYL1073

Chemical Structure : SYL1073

CAS No.: 2964520-80-5

SYL1073 (SYL 1073, SYL-1073)

Catalog No.: PC-21597Not For Human Use, Lab Use Only.

SYL1073 is a potent, selective and covalent Threonine tyrosine kinase (TTK) inhibitor with IC50 of of 16 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SYL1073 is a potent, selective and covalent Threonine tyrosine kinase (TTK) inhibitor with IC50 of of 16 nM.
SYL1073 covalently engages with TTK at the C604 residue.
SYL1073 exhibits potent anti-proliferative activity in both MDA-MB-231 (IC50 = 0.13 μM) and HCT-116 (IC50 = 0.15 μM) cell lines.
SYL1073 exhibits excellent kinase selectivity in a panel of kinases, does not inhibit five other human kinases (CHAK1, FGFR4, MAPKAPK2, MAPKAPK3 and p70S6Kβ) that feature a cysteine residue at the equivalent position as C604 in TTK kinase.
SYL1073 effectively suppresses colony formation and induce cell cycle dysregulation and apoptosis in human breast cancer cells.

Physicochemical Properties

M.Wt 471.57
Formula C25H29N9O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-(4-methyl-4H-1,2,4-triazol-3-yl)-2-((6-methyl-8-(neopentylamino)pyrido[3,4-d]pyrimidin-2-yl)amino)phenyl)acrylamide

References

1. Yaoliang Sun, et al. Bioorg Chem. 2023 Dec 25:143:107053.

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