xmd8-87

Description: XMD8-87 (also known as ACK1-B19) is a novel tyrosine kinase nonreceptor 2(TNK2) inhibitor with IC50s of 38 nmol/L and 113 nmol/L for the D163E and R806Q mutations. XMD8-87 has been reported to be potent in the inhibition of TNK2 phosphorylation. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types. XMD8-87 was identified from kinase inhibitor screens to predict functional gene targets in primary specimens from patients with acute myeloid leukemia and chronic myelomonocytic leukemia. Deep sequencing of the same patient specimens identified genetic alterations that were then integrated with the functionally important targets using the HitWalker algorithm to prioritize the mutant genes that most likely explain the observed drug sensitivity patterns.

References: Cancer Res. 2016 Jan 1; 76(1):127-38.