PIM447

• Description :

  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].

• 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.

• 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 :

  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.|Blood Adv. 2024 May 13:bloodadvances.2022008144.|Mol Cancer Ther. 2018 Apr;17 (4) :849-857.|PLoS One. 2024 Nov 1;19 (11) :e0308647.