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XMD8-87

Chemical Structure : XMD8-87

CAS No.: 1234480-46-6

XMD8-87 (Ack1 inhibitor B19)

Catalog No.: PC-35146Not For Human Use, Lab Use Only.

XMD8-87 (Ack1 inhibitor B19) is a potent Ack1 inhibitor with Kd of 15 nM, inhibits EGF-induced autophosphorylation in HEK293 cells at 2 uM.

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Biological Activity

XMD8-87 (Ack1 inhibitor B19) is a potent Ack1 inhibitor with Kd of 15 nM, inhibits EGF-induced autophosphorylation in HEK293 cells at 2 uM; completely inhibits A549 cancer cell growth, and partially inhibited EGF-stimulated cancer cell growth at 10 uM; XMD8-87 is a potent, selective Ack1 (TNK2) inhibitor with IC50 of 1.9 uM in ELISA assays; potently block proliferation of TNK2 mutant cell lines, shows IC50s of 38 nM and 113 nM for the D163E and R806Q mutations.

Physicochemical Properties

M.Wt 445.527
Formula C24H27N7O2
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

2-((2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)amino)-11-methyl-5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one

References

1. Miduturu CV, et al. Chem Biol. 2011 Jul 29;18(7):868-79.

2. Mahajan K, et al. Cancer Lett. 2013 Sep 28;338(2):185-92.

3. Maxson JE, et al. Cancer Res. 2016 Jan 1;76(1):127-38.

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