| Identification | Back Directory | [Name]
INCB053914 | [CAS]
1620012-39-6 | [Synonyms]
INCB053914
Uzansertib
Uzansertib (INCB053914)
2-Pyridinecarboxamide, N-[(7R)-4-[(3R,4R,5S)-3-amino-4-hydroxy-5-methyl-1-piperidinyl]-6,7-dihydro-7-hydroxy-5H-cyclopenta[b]pyridin-3-yl]-6-(2,6-difluorophenyl)-5-fluoro- | [Molecular Formula]
C26H26F3N5O3 | [MDL Number]
MFCD34578191 | [MOL File]
1620012-39-6.mol | [Molecular Weight]
513.51 |
| Chemical Properties | Back Directory | [Boiling point ]
642.7±55.0 °C(Predicted) | [density ]
1.444±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
3.09±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines[1]. | [in vivo]
Uzansertib (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) [1].
Uzansertib demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC50=70 nM; KMS-12-BM tumors, IC50=145 nM) [1].
| Animal Model: | Female immune compromised (severe combined immunodeficiency [SCID]) mice (5-9 weeks of age) bearing MOLM-16 (AML) or KMS-12-BM (MM)[1] | | Dosage: | 25, 50, 75, 100 mg/kg | | Administration: | PO; twice a day; for 15 days | | Result: | Inhibited tumor growth in a dose-dependent manner in mice.
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| [IC 50]
PIM1: 0.24 nM (IC50); PIM2: 30 nM (IC50); PIM3: 0.12 nM (IC50) | [References]
[1] Koblish H, et al. Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies. PLoS One. 2018 Jun 21;13(6):e0199108. DOI:10.1371/journal.pone.0199108 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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