For research use only. Not for therapeutic Use.
XMD16-5 is a potent TNK2 inhibitor with IC50 values of 16 and 77 nM for the D163E and R806Q mutations, respectively.
XMD16-5 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). XMD16-5 has IC50s of 16 nM and 77 nM for the D163E and R806Q mutations. The effects of XMD16-5 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 XMD16-5[1].
| Catalog Number | I010103 |
| CAS Number | 1345098-78-3 |
| Synonyms | 2-[4-(4-hydroxypiperidin-1-yl)anilino]-11-methyl-5H-pyrimido[4,5-b][1,4]benzodiazepin-6-one |
| Molecular Formula | C23H24N6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H24N6O2/c1-28-20-5-3-2-4-18(20)22(31)26-19-14-24-23(27-21(19)28)25-15-6-8-16(9-7-15)29-12-10-17(30)11-13-29/h2-9,14,17,30H,10-13H2,1H3,(H,26,31)(H,24,25,27) |
| InChIKey | AGLKBEPKKDHHKY-UHFFFAOYSA-N |
| SMILES | CN1C2=CC=CC=C2C(=O)NC3=CN=C(N=C31)NC4=CC=C(C=C4)N5CCC(CC5)O |
| Reference | [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. |
