| Identification | Back Directory | [Name]
SEL24-B489 | [CAS]
1616359-00-2 | [Synonyms]
SEL24
SEL24-B489
5,6-dibromo-1-isopropyl-4-nitro-2-(piperidin-4-yl)-1H-benzo[d]imidazole
1H-Benzimidazole, 5,6-dibromo-1-(1-methylethyl)-4-nitro-2-(4-piperidinyl)- | [Molecular Formula]
C15H18Br2N4O2 | [MOL File]
1616359-00-2.mol | [Molecular Weight]
446.14 |
| Chemical Properties | Back Directory | [Boiling point ]
533.2±50.0 °C(Predicted) | [density ]
1.87±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 25 mg/mL (56.04 mM; ultrasonic and adjust pH to 2 with HCl) | [form ]
Solid | [pka]
9.77±0.10(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively[1]. | [in vivo]
SEL24-B489 (25-100 mg/kg, orally) exhibited activity in AML in vivo models[1].
SEL24-B489 induces apoptosis of DLBCL cell lines in low/sub-micromolar concentrations and exhibits activity in a xenograft model[2].
| Animal Model: | SCID/beige mice bearing MV-4-11 tumors (FLT3-ITD+)[1].
| | Dosage: | 50, 75 and 100 mg/kg. | | Administration: | Orally, twice daily. | | Result: | Marked dose – dependent tumor reduction (67%, 74% and 82% tumor growth inhibition (TGI) for 50, 75 and 100 mg/kg daily doses, respectively). |
| [IC 50]
PIM1: 2 nM (Kd); PIM2: 2 nM (Kd); PIM3: 3 nM (Kd); FLT3-ITD | [References]
[1] Wojciech Czardybon, A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia. Oncotarget. 2018 Mar 30;9(24):16917-16931. DOI:10.18632/oncotarget.24747
[2] Ewa Jablonska, et al. A Novel Pan-PIM Kinase Inhibitor, SEL24-B489, Induces Apoptosis and Inhibits Proliferation of Diffuse Large B-Cell Lymphoma Cells through Inhibition of Protein Translation and Attenuation of Myc and NFkB Activity. Blood (2015) 126 (2 |
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