XMD 8-87

Discontinued Product

XMD 8-87 (Cat. No. 6061) has been withdrawn from sale for commercial reasons.
Description: Potent Ack1/TNK2 inhibitor
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
Purity: ≥98% (HPLC)
Literature (3)

Biological Activity for XMD 8-87

XMD 8-87 is a 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 for XMD 8-87

M. Wt 445.52
Formula C24H27N7O2
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1234480-46-6
PubChem ID 53322923
Smiles COC1=C(C=CC(N2CCN(CC2)C)=C1)NC3=NC=C4NC(C5=CC=CC=C5N(C4=N3)C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

References for XMD 8-87

References are publications that support the biological activity of the product.

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, XMD 8-87 supplier, XMD8-87, Inhibitors, inhibits, Ack1, TNK2, Ba/F3, leukemia, D163E, R806Q, phosphorylation, tyrosine, kinase, 2, 6061, Tocris Bioscience

Citations for XMD 8-87

Citations are publications that use Tocris products.

Currently there are no citations for XMD 8-87.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Epigenetics Scientific Review

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Cancer Metabolism Poster

Cancer Metabolism Poster

This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.