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A-420983

Chemical Structure : A-420983

CAS No.: 330789-03-2

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A-420983 (A420983)

Catalog No.: PC-20792Not For Human Use, Lab Use Only.

A-420983 is a potent, orally active inhibitor of Lck kinase with IC50 of 37 nM, inhibits whole blood IL-2 production with IC50 of 7 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A-420983 is a potent, orally active inhibitor of Lck kinase with IC50 of 37 nM, inhibits whole blood IL-2 production with IC50 of 7 nM.
A-420983 also potently inhibits Src with IC50 of 70 nM, displays >500-fold selectivity over KDR and >25-fold selectivity over Tie-2.
A-420983 exhibits oral efficacy in animal models of delayed-type hypersensitivity and organ transplant rejection.

Physicochemical Properties

M.Wt 593.74
Formula C33H39N9O2
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-(4-(4-amino-1-((1r,4r)-4-(4-methylpiperazin-1-yl)cyclohexyl)-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-methoxyphenyl)-1-methyl-1H-indole-2-carboxamide

References

1. David W Borhani, et al. Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6.

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