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PIM447

CAT: 0804-HY-19322-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-19322-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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.

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