For research use only. Not for therapeutic Use.
TP-5801 is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity[1].
TP-5801 (10 pM-10 μM; 72 h) treatment inhibits TNK1-driven, BCR-ABL-driven and IL-3-driven Ba/F3 cell growth[1].
TP-5801 (1 nM-10 μM; 10 d) inhibits TNK1-dependent L540 cell growth[1].
TP-5801 (oral gavage; 10 mg/kg; once) treatment shows efficacy in the mouse survival model[1].
TP-5801 (oral gavage; 50 mg/kg; once daily; 7 d) treatment can inhibit localized tumor growth[1].
| Catalog Number | I043384 |
| CAS Number | 2574474-81-8 |
| Synonyms | 5-bromo-4-N-[2-(dimethylamino)pyridin-3-yl]-2-N-[2-methoxy-5-methyl-4-(4-methylpiperazin-1-yl)phenyl]pyrimidine-2,4-diamine |
| Molecular Formula | C24H31BrN8O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H31BrN8O/c1-16-13-19(21(34-5)14-20(16)33-11-9-32(4)10-12-33)29-24-27-15-17(25)22(30-24)28-18-7-6-8-26-23(18)31(2)3/h6-8,13-15H,9-12H2,1-5H3,(H2,27,28,29,30) |
| InChIKey | CPJOTOBXAWKVCT-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C=C1N2CCN(CC2)C)OC)NC3=NC=C(C(=N3)NC4=C(N=CC=C4)N(C)C)Br |
| Reference | [1]. Tsz-Yin Chan, et al. TNK1 is a ubiquitin-binding and 14-3-3-regulated kinase that can be targeted to block tumor growth. Nat Commun. 2021 Sep 9;12(1):5337. |
