SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with K d values of 2 nM for PIM1 , 2 nM for PIM2 and 3 nM for PIM3 , respectively In Vitro In MOLM-13 and to a lesser extent in MV4-11 cells, a dose-dependent disruption of cell cycle with especially pronounced depletion of the S phase after treatment with SEL24-B489, accompanied by PARP cleavage and apoptosis was observed. SEL24-B489 causes a profound inhibition of S6 (S 235/236 ), but has little effect on PI3K/mTOR signaling. SEL24-B489 inhibits STAT5 (Ser 726 ) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: AZD1208, AC220 and AraC in AML cell lines. Concentration: 0-10 μM. Incubation Time: 72 h. Result: Decreased viability. In Vivo SEL24-B489 (25-100 mg/kg, orally) exhibited activity in AML in vivo models . SEL24-B489 induces apoptosis of DLBCL cell lines in low/sub-micromolar concentrations and exhibits activity in a xenograft model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID/beige mice bearing MV-4-11 tumors (FLT3-ITD+) . 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). Form:Solid IC50& Target:PIM1 2 nM (Kd) PIM2 2 nM (Kd) PIM3 3 nM (Kd) FLT3-ITD
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SEL24-B489
CAS number：1616359-00-2 molecular formula：C15H18Br2N4O2
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| Chinese alias | - | ||
| English alias | AKOS040756928 | SEL24-B289 | UNII-9M7X64VTLI | 9M7X64VTLI | Pim/flt3 kinase inhibitor SEL24 | SEL-24 free base | 5,6-Dibromo-1-(1-methylethyl)-4-nitro-2-(4-piperidinyl)-1H-benzimidazole | SEL 24 [WHO-DD] | SCHEMBL15826208 | 5,6-Dibromo-4-nitro-2-(piperidi | ||
| CAS number | 1616359-00-2 | molecular formula | C15H18Br2N4O2 |
| molecular weight | 446.14 g/mol | Exact mass | ≥98% |
| PSA | - | logp | - |
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