SEL24-B489

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SEL24-B489 

SEL24-B489 是有效的、I 型的、口服有效的、PIM 和 FLT3-ITD 的双抑制剂，其对PIM1、PIM2 和 PIM3 的 Kd 值分别为 2 nM、2 nM、和 3 nM。

SEL24-B489

SEL24-B489 Chemical Structure

CAS No. : 1616359-00-2

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生物活性

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].

IC50 & Target[1]

PIM1

2 nM (Kd)

PIM2

2 nM (Kd)

PIM3

3 nM (Kd)

FLT3-ITD

 

体外研究
(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[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd 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+)[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).

分子量

446.14

Formula

C15H18Br2N4O2
CAS 号

1616359-00-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

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