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MEN1703

Chemical Structure : MEN1703

CAS No.: 1616359-00-2

MEN1703 (SEL24-B489, SEL24)

Catalog No.: PC-63507Not For Human Use, Lab Use Only.

SEL24-B489 (SEL24, MEN1703) is a potent, dual PIM and FLT3-ITD inhibitor with Kd of 2/2/3 nM for PIM1/2/3, Kd of 160/16 nM for FLT3-WT/FLT3-ITD, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SEL24-B489 (SEL24, MEN1703) is a potent, dual PIM and FLT3-ITD inhibitor with Kd of 2/2/3 nM for PIM1/2/3, Kd of 160/16 nM for FLT3-WT/FLT3-ITD, respectively.
SEL24-B489 exhibits significantly broader on-target activity in AML cell lines (MV-4-11 GI50=20 nM) and primary AML blasts than selective FLT3-ITD or PIM inhibitors.
SEL24-B489 decreases viability of AML cells with FLT3-TKD mutations associated with resistance to selective FLT3-ITD inhibitors.
SEL24-B489 inhibits the growth of a broad panel of AML cell lines in xenograft models.

Physicochemical Properties

M.Wt 446.143
Formula C15H18Br2N4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5,6-dibromo-4-nitro-2-(piperidin-4-yl)-1-(propan-2-yl)-1H-1,3-benzodiazole

References

1. Czardybon W, et al. Oncotarget. 2018 Mar 30;9(24):16917-16931.

2. Białopiotrowicz E, et al. J Cell Mol Med. 2018 Apr 17. doi: 10.1111/jcmm.13632.

3. Szydłowski M, et al. Blood. 2017 Sep 21;130(12):1418-1429.

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