475857

Mirk/Dyrk1B Inhibitor, Compound A

• Synonym(s): Mirk/Dyrk1B Inhibitor, Compound A, N-(2-Chloro-5-(3-chlorobenzylcarbamoyl)phenyl)-2-methoxy-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carboxamide, N-(2-Chloro-5-((3-chlorobenzyl)carbamoyl)phenyl)-7-hydroxy-2-methoxypyrido[2,3-d]pyrimidine-6-carboxamide
• Empirical Formula (Hill Notation): C₂₃H₁₇Cl₂N₅O₄
• Molecular Weight: 498.32
• UNSPSC Code: 12352200

Properties

• assay: ≥99% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 2 mg/mL
• shipped in: wet ice
• storage temp.: 2-8°C

Description

General description

A cell-permeable dihydropyridopyrimidine-carboxamide compound that acts as a potent and reversible inhibitor of Mirk/Dyrk1B and Dyrk1A kinases (IC₅₀ = 68 and 22 nM). Exhibits very high selectivity for Mirk/Dyrk1B compared to Abl, Flt3, and MARK1 (64, 56 and 73% inhibition at 10 µM, respectively) and a panel of 46 other kinases. Shown to induce activation of caspase-3 and sensitize tumor cells to the action of gemcitabine and cisplatin (Cat. No. 232120), possibly by de-stabilizing p27. Preferentially increases cycling in Mirk-elevated quiescent pancreatic cancer cells (SU86.86, Panc1, AsPc1, and SW620 at ~1 µM). Also, shown to increase level of superoxides in quiescent pancreatic tumor cells (Panc1, SU86.86, and AsPc1) by blocking SOD2 and SOD3 activities.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C), Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Ewton, D.Z., et al. 2011. Mol. Cancer Ther.10, 2104.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable