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515846-21-6

515846-21-6 Structure

515846-21-6 Structure
IdentificationBack Directory
[Name]

SP 4206
[CAS]

515846-21-6
[Synonyms]

SP 4206
[Molecular Formula]

C30H37Cl2N7O6
[MDL Number]

MFCD34469270
[MOL File]

515846-21-6.mol
[Molecular Weight]

662.56
Chemical PropertiesBack Directory
[density ]

1.47±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[form ]

Solid
[pka]

3.05±0.10(Predicted)
[color ]

White to light yellow
Hazard InformationBack Directory
[Definition]

ChEBI: N(2)-carbamimidoyl-N-{2-[4-(3-{4-[(5-carboxyfuran-2-yl)methoxy]-2,3-dichlorophenyl}-1-methyl-1H-pyrazol-5-yl)piperidin-1-yl]-2-oxoethyl}-D-leucinamide is a leucine derivative obtained by fpormal condensation of the secondary amino group of 5-({2,3-dichloro-4-[1-methyl-5-(piperidin-4-yl)-1H-pyrazol-3-yl]phenoxy}methyl)-2-furoic acid and the carboxy group of N-amidino-L-leucylglycine It is a member of guanidines, a furoic acid, a pyrazolylpiperidine, a glycine derivative, a dichlorobenzene and a D-leucine derivative.
[Biological Activity]

SP4206 is an IL-2/IL-2Rα interaction inhibitor. SP4206 binds with high affinity (Kd=70 nM) to IL-2 and blocks binding to its natural receptor IL-2Rα (Kd=10 nM)[1]. SP4206 binds the WT IL-2, IL-2 variant K35L/M39V, IL-2 variant P65A, and IL-2 variant V69A with EC50s of 68.8, 80.1, 117.0, and 10.4 nM, respectively[1].
[References]

[1]. Thanos CD, et al. Hot-spot mimicry of a cytokine receptor by a small molecule. Proc Natl Acad Sci U S A. 2006 Oct 17;103(42):15422-7.
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