XMD 8-87

Cat. No. 6061new

XMD 8-87 C24H27N7O2 [1234480-46-6]

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Chemical Name: 5,11-Dihydro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-11-methyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one

Biological Activity

Potent Ack1/TNK2 inhibitor (IC50 = 38 and 113 nM in Ba/F3 cell lines containing leukemia-associated D163E and R806Q mutations respectively). Blocks phosphorylation of TNK2 receptors containing solid-tumor type truncation mutations.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M.Wt:
445.52
Formula:
C24H27N7O2
Solubility:
Soluble to 100 mM in 1eq. HCl and to 50 mM in DMSO
Purity:
>98 %
Storage:
Store at RT
CAS No:
1234480-46-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Maxson et al (2015) Identification and characterization of tyrosine kinase nonreceptor 2 mutations in leukemia through integration of kinase inhibitor screening and genomic analysis. Cancer.Res. 76 127. PMID: 26677978.

Maxson et al (2014) Development and repurposing of small-molecule kinase inhibitors to target novel leukemogenic TNK2 mutations Blood 124 435.

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Keywords: XMD 8-87, supplier, XMD8-87, Inhibitors, inhibits, Ack1, TNK2, Ba/F3, leukemia, D163E, R806Q, phosphorylation, tyrosine, kinase, 2, Tocris Bioscience, Ack1 Inhibitor products

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