PIM-447 (dihydrochloride)

• UNSPSC Description:

  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].

• Target Antigen:

  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 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 20Blood Adv. 2024 May 13:bloodadvances.2022008144.|Mol Cancer Ther. 2018 Apr;17(4):849-857.|bioRxiv. 2024 Mar 28.|bioRxiv. 2024 October 24.|Cell Chem Biol. 2023 Nov 16:S2451-9456(23)00384-7.|J Pathol. 2020 Sep;252(1):65-76.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

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

• Clinical Information:

  Phase 1

• CAS Number:

  1820565-69-2