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GSK 2830371

Cat. No. M6770
GSK 2830371 Structure
Size Price Availability Quantity
10mg USD 98  USD98 In stock
50mg USD 315  USD315 In stock
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Quality Control & Documentation
Biological Activity

GSK 2830371 is a potent and selective allosteric inhibitor of Wip1 phosphatase (IC50 = 6 nM). Exhibits selectivity for Wip1 over 21 other phosphatases. Increases phosphorylation of Wip1 substrates, including p53, Chk2, H2AX and ATM. Attenuates tumor cell growth in a variety of lymphoid cell lines. Also inhibits lymphoma xenograft growth in vivo. Orally bioavailable.

Chemical Information
Molecular Weight 461.02
Formula C23H29ClN4O2S
CAS Number 1404456-53-6
Form Solid
Solubility (25°C) DMSO 46.1 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] Berger, et al. Naunyn Schmiedebergs Arch Pharmacol. Inhibition of potassium outward currents and pacemaker current in sheep cardiac Purkinje fibres by the verapamil derivative YS-035.

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  Catalog
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Keywords: GSK 2830371 supplier, Phosphatase, inhibitors, activators


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