Product 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].
Applications: Cancer-Kinase/protease
Formula: C24H25Cl2F3N4O
Citations: Blood 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.
References: [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
CAS Number: 1820565-69-2
Molecular Weight: 513.38
Compound Purity: 99.94
Research Area: Cancer
Solubility: DMSO : ≥ 46.7 mg/mL/H2O : 50 mg/mL (ultrasonic)
Target: Apoptosis;Pim
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