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TCS PIM-1 1

Cat. No. M3745
TCS PIM-1 1 Structure
Size Price Availability Quantity
10mg USD 105 In stock
50mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

TCS PIM-1 1 is a potent, ATP-competitive inhibitor of Pim-1 kinase. This compound displays selectivity over Pim-2 and MEK1/MEK2 (IC50 values are 50, >20000 and >20000 nM for Pim-1, Pim-2, and MEK1/MEK2, respectively). TCS PIM-1 1 bound convincingly within the ATP-binding site of Pim-1 suggesting an ATP-competitive inhibitory mechanism.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 367.2
Formula C18H11BrN2O2
CAS Number 491871-58-0
Purity >99%
Solubility DMSO
Storage at -20°C
References

Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
Cheney IW, et al. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83. PMID: 17251021.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TCS PIM-1 1 supplier, Pim, inhibitors

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