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SEL24-B489

Catalog No. T39085 CAS 1616359-00-2

Synonyms: SEL24-B489

SEL24-B489 is a highly effective and orally bioavailable compound that acts as a robust, type I inhibitor of both PIM and FLT3-ITD. It exhibits exceptional binding affinity with K d values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3.

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SEL24-B489, CAS 1616359-00-2

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	SEL24-B489 is a highly effective and orally bioavailable compound that acts as a robust, type I inhibitor of both PIM and FLT3-ITD. It exhibits exceptional binding affinity with K d values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3.
Targets&IC50	Pim1:2 nM (Kd), Pim3:3 nM (Kd), Pim2:2 nM (Kd)
In vitro	In MOLM-13 and, to a lesser extent, MV4-11 cells, SEL24-B489 prompts a dose-dependent disruption of the cell cycle, notably depleting the S phase, leading to PARP cleavage and apoptosis[1]. Moreover, SEL24-B489 significantly inhibits S6 (S 235/236) while minimally affecting PI3K/mTOR signaling[1]. It also suppresses STAT5 (Ser 726) and reduces MCL1 expression without altering c-MYC levels or prompting PARP cleavage, unlike selective inhibitors[1]. In a Cell Viability Assay[1] using AML cell lines with AZD1208, AC220, and AraC at 0-10 μM concentrations over 72 hours, a noticeable decline in cell viability was observed.
In vivo	SEL24-B489, when administered orally at doses ranging from 25-100 mg/kg, demonstrated effectiveness against Acute Myeloid Leukemia (AML) in vivo[1]. Additionally, it effectively induced apoptosis in Diffuse Large B-Cell Lymphoma (DLBCL) cell lines at low/sub-micromolar concentrations and showed efficacy in a xenograft model[2]. In an animal study using SCID/beige mice implanted with MV-4-11 tumors (FLT3-ITD+), doses of 50, 75, and 100 mg/kg given orally twice daily resulted in significant, dose-dependent tumor reduction, achieving 67%, 74%, and 82% tumor growth inhibition (TGI) for the respective daily doses[1].

Synonyms	SEL24-B489
Molecular Weight	446.143
Formula	C15H18Br2N4O2
CAS No.	1616359-00-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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. 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 (23): 706.

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Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SEL24-B489 1616359-00-2 SEL24-B 489 SEL24B489 SEL-24-B489 SEL24-B-489 SEL24 B489 inhibitor inhibit

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