| Identification | Back Directory | [Name]
2,4-Pyrimidinediamine, 5-bromo-N4-[2-(dimethylamino)-3-pyridinyl]-N2-[2-methoxy-5-methyl-4-(4-methyl-1-piperazinyl)phenyl]- | [CAS]
2574474-81-8 | [Synonyms]
TP-5801
2,4-Pyrimidinediamine, 5-bromo-N4-[2-(dimethylamino)-3-pyridinyl]-N2-[2-methoxy-5-methyl-4-(4-methyl-1-piperazinyl)phenyl]- | [Molecular Formula]
C24H31BrN8O | [MOL File]
2574474-81-8.mol | [Molecular Weight]
527.46 |
| Chemical Properties | Back Directory | [Boiling point ]
668.5±65.0 °C(Predicted) | [density ]
1.391±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
7.75±0.42(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Uses]
TP-5801 is an orally active TNK1 (non-receptor tyrosine kinase) inhibitor (IC50=1.40 nM), and shows anti-tumor activity[1]. | [in vivo]
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]. | Animal Model: | Female NOD/SCID mice injected with Ba/F3 luc cells expressing TNK1 AAA[1] | | Dosage: | 10 mg/kg | | Administration: | Oral gavage; 10 mg/kg; once | | Result: | Showed no signs of toxicity and significantly prolonged lifespan. |
| Animal Model: | NOD/SCID mice implanted subcutaneously with Ba/F3 luc cells expressing TNK1 AAA or BCR-ABL[1] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage; 50 mg/kg; once daily; 7 days | | Result: | Reduced phospho-STAT3 in TNK1-driven xenografts at 2?hours post-treatment, and tumor burden in mice xenografted. |
| [References]
[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. DOI:10.1038/s41467-021-25622-3 |
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