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XMD 8-87

Names

[ CAS No. ]:
1234480-46-6

[ Name ]:
XMD 8-87

[Synonym ]:
6H-Pyrimido[4,5-b][1,4]benzodiazepin-6-one, 5,11-dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-11-methyl-
2-{[2-Methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino}-11-methyl-5,11-dihydro-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
XMD8-87

Biological Activity

[Description]:

XMD8-87 is a potent TNK2 inhibitor with IC50 values of 38 and 113 nM for the D163E and R806Q mutations, respectively.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Tyrosinase
Research Areas >> Cancer

[Target]

IC50: 38 nM (TNK2, D163E mutation), 113 nM (TNK2, R806Q mutation)[1]


[In Vitro]

XMD8-87 potently inhibits the growth of the TNK2 mutant expressing cell lines while having little or no effect on the control cells out to the highest tested concentrations (1,000 nM). XMD8-87 has IC50s of 38 nM and 113 nM for the D163E and R806Q mutations. The effects of XMD8-87 on TNK2 cell lines are largely due to on-target effects on TNK2. Auto-phosphorylation of overexpressed TNK2 mutants could be blocked with TNK2 inhibitor XMD8-87[1].

[Kinase Assay]

Kinase targets are tested with biochemical enzymatic kinase assays using the SelectScreen Kinase Profiling Service to determine IC50 values. The compounds (XMD8-87) are assayed at 10 concentrations (3-fold serial dilutions starting from 1 μM) at an ATP concentration equal to the ATP Km[1].

[Cell Assay]

Cells are treated with the following inhibitors for 72 hours: dasatinib, AIM-100, XMD8-87 and XMD16-5. Cell viability is measured using a methanethiosulfonate (MTS)-based assay and absorbance (490 nm) is read at 1 and 3 hours after adding reagent[1].

[References]

[1]. Maxson JE, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis.


[Related Small Molecules]

Taxifolin | XMD16-5 | Mulberroside A | Arbutin | Oxyresveratrol | Deoxyarbutin | 4-Hexylresorcinol | 4-Butylresorcinol | Glycolic acid

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C24H27N7O2

[ Molecular Weight ]:
445.517

[ Exact Mass ]:
445.222626

[ LogP ]:
1.23

[ Index of Refraction ]:
1.648

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds