2574474-81-8

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
Molecular Formula	C24H31BrN8O
Molecular Weight	527.46
MOL File	2574474-81-8.mol

Synonyms

TP-5801 2,4-Pyrimidinediamine, 5-bromo-N4-[2-(dimethylamino)-3-pyridinyl]-N2-[2-methoxy-5-methyl-4-(4-methyl-1-piperazinyl)phenyl]-

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Chemical Properties

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

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

Supplier

Shanghai Beckham Medical Technology Co., Ltd

Telephone 13816613772

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16976/0_EN.htm

Guangzhou Younan Technology Co., Ltd

Telephone020-82000279 18988941452

Websitehttp://www.ubiochem.cn/

Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd

Telephone 15317229551

Websitehttps://www.ureiko.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Aikon International Limited

Telephone025-58859352 18651614124

Websitehttps://www.aikonchem.com/

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