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SEL24-B489

Catalog No.GC64774

SEL24-B489 es un potente inhibidor dual de PIM y FLT3-ITD de tipo I, activo por vÍa oral, con valores de Kd de 2 nM para PIM1, 2 nM para PIM2 y 3 nM para PIM3, respectivamente.

Products are for research use only. Not for human use. We do not sell to patients.

SEL24-B489 Chemical Structure

Cas No.: 1616359-00-2

Tamaño Precio Disponibilidad Cantidad
5 mg
450,00 $
Disponible
10 mg
765,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description of SEL24-B489

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 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].

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].

[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.

Chemical Properties of SEL24-B489

Cas No. 1616359-00-2 SDF
Formula C15H18Br2N4O2 M.Wt 446.14
Solubility DMSO : 25 mg/mL (56.04 mM; ultrasonic and adjust pH to 2 with HCl) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SEL24-B489

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1 mg 5 mg 10 mg
1 mM 2.2414 mL 11.2072 mL 22.4145 mL
5 mM 0.4483 mL 2.2414 mL 4.4829 mL
10 mM 0.2241 mL 1.1207 mL 2.2414 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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