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SEL24-B489

产品编号 T39085 CAS 1616359-00-2

别名: 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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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	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.
靶点活性	Pim1:2 nM (Kd), Pim3:3 nM (Kd), Pim2:2 nM (Kd)
体外活性	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 (S 235/236 ), but has little effect on PI3K/mTOR signaling[1]. 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[1]. Cell Viability Assay[1]Cell Line: AZD1208, AC220 and AraC in AML cell lines. Concentration: 0-10 μM. Incubation Time: 72 h. Result: Decreased viability.
体内活性	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).

别名	SEL24-B489
分子量	446.143
分子式	C15H18Br2N4O2
CAS No.	1616359-00-2

存储

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

计算器

摩尔浓度计算器

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参考文献

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.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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