Mirk/Dyrk1B Inhibitor, Compound A

Name: Mirk/Dyrk1B Inhibitor, Compound A
Brand: MM

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

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About This Item

Empirical Formula (Hill Notation):

C₂₃H₁₇Cl₂N₅O₄

Molecular Weight:

498.32

UNSPSC Code:

12352200

assay

≥99% (HPLC)

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

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

Other Notes

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

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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