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XMD 8-87
Axon 2762
CAS:
1234480-46-6
Purity:
98%
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C24H27N7O2
- MW: 445.52
Description
XMD8-87 (ACK1-B19) is a potent ATP-competitive inhibitor of ACK1/TNK2, with a reported Kd value of 15 nM. It inhibits leukemia-associated TNK2 variants with IC50 values of 38 nM for D163E and 113 nM for R806Q.
ACK1 is a nonreceptor tyrosine kinase involved in growth-factor signaling, cell attachment, migration and oncogenic pathway activation. XMD8-87 is used to investigate wild-type and mutant TNK2 signaling, kinase dependence and downstream effects on proliferation and invasive behavior.
Key Features
- Potent ACK1/TNK2 inhibitor
- Kd: 15 nM
- IC50: 38 nM for D163E and 113 nM for R806Q
- ATP-competitive and reversible mechanism
Applications
- ACK1/TNK2 kinase research
- Oncogenic TNK2 mutation studies
- Kinase target-engagement assays
- Cell migration and invasion research
- Leukemia signaling models
More Information
| Parent CAS No. | 1234480-46-6 |
|---|---|
| Chemical Name | 2-(2-Methoxy-4-(4-methylpiperazin-1-yl)phenylamino)-11-methyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one |
| SMILES | C1(OC)C(NC2N=CC3NC(=O)C4C=CC=CC=4N(C)C=3N=2)=CC=C(N2CCN(C)CC2)C=1 |
| MFCD | N.A. |
| InChi | InChI=1S/C24H27N7O2/c1-29-10-12-31(13-11-29)16-8-9-18(21(14-16)33-3)27-24-25-15-19-22(28-24)30(2)20-7-5-4-6-17(20)23(32)26-19/h4-9,14-15H,10-13H2,1-3H3,(H,26,32)(H,25,27,28) |
| InChiKey | LGLHCXISMKHLIK-UHFFFAOYSA-N |
| CID | 53322923 |
| Short Description | Ack1 inhibitor |
References
- JE Maxson et al. Development and Repurposing of Small-Molecule Kinase Inhibitors to Target Novel Leukemogenic TNK2 Mutations. Blood 2014 124:435.
- JE Maxson et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis. Cancer Res. 2016 Jan 1;76(1):127-38.
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