PIM447

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[1][2].

Product Specifications

CAS Number

[1210608-43-7]

Product Name Alternative

LGH447

UNSPSC

12352005

Hazard Statement

H301-H311-H331

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/PIM447.html

Concentration

10mM

Purity

99.52

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(C1=CC=C(F)C(C2=C(F)C=CC=C2F)=N1)NC3=C([C@@H]4C[C@H](C)C[C@H](N)C4)C=CN=C3

Molecular Formula

C24H23F3N4O

Molecular Weight

440.46

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P361-P403+P233-P405-P501

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]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|[3]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.