EF-4-177

Chemical Structure : EF-4-177

Catalog No.: PC-49698Not For Human Use, Lab Use Only.

EF-4-177 is a potent, selective, allosteric and orally active CDK2 inhibitor with ITC KD of 7.4 nM.
EF-4-177 binds CDK2 in a manner that is negatively cooperative with cyclin binding.

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Biological Activity

EF-4-177 is a potent, selective, allosteric and orally active CDK2 inhibitor with ITC KD of 7.4 nM.
EF-4-177 binds CDK2 in a manner that is negatively cooperative with cyclin binding.
EF-4-177 is selective for CDK2 over structurally similar CDK1, showing the promise of targeting the allosteric pocket to achieve selectivity.
EF-4-177 significantly decreased sperm count in CD-1 mice after the 28 day exposure.

Physicochemical Properties

M.Wt	431.38
Formula	C18H14F5N3O2S
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	OC(C1=CC(S(F)(F)(F)(F)F)=CC=C1NCCC2=CNC3=C2C=CC(C#N)=C3)=O

References

1. Erik B Faber, et al. J Med Chem. 2023 Jan 26. doi: 10.1021/acs.jmedchem.2c01731.

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EF-4-177

Biological Activity

Physicochemical Properties

References

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