| Bioactivity | 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]. | ||||||||||||
| Invitro | 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[1].SEL24-B489 causes a profound inhibition of S6 (S235/236), but has little effect on PI3K/mTOR signaling[1].SEL24-B489 inhibits STAT5 (Ser726) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| Name | SEL24-B489 | ||||||||||||
| CAS | 1616359-00-2 | ||||||||||||
| Formula | C15H18Br2N4O2 | ||||||||||||
| Molar Mass | 446.14 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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