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TC-S 7004

Cat. No. M7390
TC-S 7004 Structure
Synonym:

Dyrk1B/A-IN-1

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Quality Control & Documentation
Biological Activity

TC-S 7004 is a potent and selective DYRK1A/B inhibitor (IC50 values are 22 and 68 nM respectively). Selective for DYRK1A/B over a panel of other kinases. Reduces accumulation of quiescent Panc1 pancreatic cancer cells in G0 under serum free conditions. Also induces DNA damage and apoptosis in quiescent Panc1 cells.

Chemical Information
Molecular Weight 498.32
Formula C23H17Cl2N5O4
CAS Number 1386979-55-0
Solubility (25°C) DMSO 49.83 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Barberis and Tribolle. Crit Rev Neurobiol. Vasopressin and oxytocin receptors in the central nervous system.

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Keywords: TC-S 7004, Dyrk1B/A-IN-1 supplier, inhibitors, activators


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