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Pim-1 kinase inhibitor 5

Cat. No. M42106
Pim-1 kinase inhibitor 5 Structure
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Biological Activity

Pim-1 kinase inhibitor 5 is a Pim-1 kinase inhibitor (IC50: 0.61 μM).

Chemical Information
Molecular Weight 406.26
Formula C22H13Cl2N3O
CAS Number 2928606-67-9
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] Anne-Sophie Castanet et al. Eur J Med Chem. Discovery of PIM-1 kinase inhibitors based on the 2,5-disubstituted 1,3,4-oxadiazole scaffold against prostate cancer: Design, synthesis, in vitro and in vivo cytotoxicity investigation

[2] Mirosława Koronkiewicz et al. BMC Cancer. Antitumor activity of the protein kinase inhibitor 1-(β-D-2'-deoxyribofuranosyl)-4,5,6,7-tetrabromo- 1H-benzimidazole in breast cancer cell lines

[3] Mostafa M M El-Miligy et al. Bioorg Chem. Discovery of small molecule acting as multitarget inhibitor of colorectal cancer by simultaneous blocking of the key COX-2, 5-LOX and PIM-1 kinase enzymes

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

[5] Jin-Dong Liu et al. Chin Med J (Engl). Pim-1 Kinase Regulating Dynamics Related Protein 1 Mediates Sevoflurane Postconditioning-induced Cardioprotection

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Keywords: Pim-1 kinase inhibitor 5 supplier, Pim, inhibitors, activators

 
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