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PIM447

Cat. No. M27950
PIM447 Structure
Synonym:

LGH447

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Quality Control & Documentation
Biological Activity

PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.

Chemical Information
Molecular Weight 440.46
Formula C24H23F3N4O
CAS Number 1210608-43-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Jian Wu, et al. Cancers (Basel). PIM Kinases in Multiple Myeloma

[2] Nikita Wadhwani, et al. J Pediatr Surg. PIM447 inhibits oncogenesis and potentiates cisplatin effects in hepatoblastoma

[3] Shinsuke Iida, et al. Int J Hematol. A phase I, dose-escalation study of oral PIM447 in Japanese patients with relapsed and/or refractory multiple myeloma

[4] Teresa Paíno, et al. Cancers (Basel). Protein Translation Inhibition is Involved in the Activity of the Pan-PIM Kinase Inhibitor PIM447 in Combination with Pomalidomide-Dexamethasone in Multiple Myeloma

[5] Teresa Paíno, et al. Clin Cancer Res. The Novel Pan-PIM Kinase Inhibitor, PIM447, Displays Dual Antimyeloma and Bone-Protective Effects, and Potently Synergizes with Current Standards of Care

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  Catalog
Abmole Inhibitor Catalog




Keywords: PIM447, LGH447 supplier, Pim, inhibitors, activators


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