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PIM-447 (dihydrochloride)

PIM447 dihydrochloride (LGH447 dihydrochloride) 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 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis[1][2].

Product Specifications

CAS Number

1820565-69-2

Product Name Alternative

LGH447 dihydrochloride

UNSPSC

12352005

Target

Apoptosis; Pim

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PIM-447-dihydrochloride.html

Purity

99.94

Solubility

DMSO : ≥ 46.7 mg/mL|H2O : 50 mg/mL (ultrasonic)

Smiles

O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=C([C@H]4C[C@@H](N)C[C@@H](C)C4)C=CN=C3.Cl.Cl

Molecular Formula

C24H25Cl2F3N4O

Molecular Weight

513.38

References & Citations

[1]Paíno T et al. The novel pan-PIM kinase inhibitor, PIM447, displays dual anti-myeloma and bone protective effects, and potently synergizes with current standards of care. Clin Cancer Res. 2016 Jul 20.|[2]Burger MT et al. Identification of N- (4- ((1R,3S,5S) -3-Amino-5-methylcyclohexyl) pyridin-3-yl) -6- (2,6-difluorophenyl) -5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. 
 J Med Chem. 2015 Nov 12;58 (21) :8373-86.|[3]Peters TL et al. Control of translational activation by PIM kinase in activated B-cell diffuse large B-cell lymphoma confers sensitivity to inhibition by PIM447.
 Oncotarget. 2016 Aug 20

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

PIM1; PIM2; PIM3

Citation 01

Blood Adv. 2024 May 13:bloodadvances.2022008144.|Mol Cancer Ther. 2018 Apr;17 (4) :849-857.|PLoS One. 2024 Nov 1;19 (11) :e0308647.|bioRxiv. 2024 Mar 28.|bioRxiv. 2024 October 24.|Cell Chem Biol. 2024 Feb 15;31 (2) :326-337.e11.|J Pathol. 2020 Sep;252 (1) :65-76.

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