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Pim-1 kinase inhibitor 4

Cat. No. M42105
Pim-1 kinase inhibitor 4 Structure
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Biological Activity

Pim-1 kinase inhibitor 4 is a Pim-1 kinase inhibitor (IC50: 17.01 nM).

Chemical Information
Molecular Weight 333.77
Formula C19H12ClN3O
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] Francesco Casuscelli et al. Chirality. Stereoselective synthesis of 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives as PIM kinase inhibitors inspired from marine alkaloids

[2] Jiwei Xu et al. Bioorg Med Chem Lett. Design, synthesis, and bioactivity evaluation of macrocyclic benzo[b]pyrido[4,3-e][1,4]oxazine derivatives as novel Pim-1 kinase inhibitors

[3] Yanghwan Yun et al. Chem Pharm Bull (Tokyo). 2-Thioxothiazolidin-4-one Analogs as Pan-PIM Kinase Inhibitors

[4] Seham S El-Hawary et al. Front Chem. New Pim-1 Kinase Inhibitor From the Co-culture of Two Sponge-Associated Actinomycetes

[5] Carmen Blanco-Aparicio et al. Cancer Lett. Pim 1 kinase inhibitor ETP-45299 suppresses cellular proliferation and synergizes with PI3K inhibition

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Keywords: Pim-1 kinase inhibitor 4 supplier, Pim, inhibitors, activators

 
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