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INCB053914

  Cat. No.:  DC10918  
Chemical Structure
1620012-39-6
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More than 5000 active chemicals with high quality for research!
Field of application
INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.
Cas No.: 1620012-39-6
Chemical Name: N-((R)-4-((3R,4R,5S)-3-amino-4-hydroxy-5-methylpiperidin-1-yl)-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
Synonyms: INCB-053914
SMILES: C(C(NC1=CN=C2[C@@H](O)CCC2=C1N1C[C@@H](C)[C@H](O)[C@@H](N)C1)=O)1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1
Formula: C26H26F3N5O3
M.Wt: 513.521
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively; INCB053914 is highly selective against a panel of more than 50 kinases (>475-fold selectivity) with exception of RSK2 (IC50=7.1 uM); inhibits cellular proliferation in a panel of cell lines derived from hematologic malignancies including AML, MM, DLBCL, MCL, and T-ALL with GI50 of <100 nM, inhibits proliferation in all MM cell lines with GI5050 of 13.2-230.0 nM; inhibits PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells with IC50 of 4 and 27 nM, also increases PIM2 expression in KG-1a (AML), Pfeiffer, and KMS12-PE cells; in vivo, INCB053914 inhibited Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC10918 INCB053914 INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively.
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