TP-5801 | TNK1 inhibitor | Probechem Biochemicals

Chemical Structure : TP-5801

CAS No.: 2574474-81-8

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TP-5801 (TP5801)

货号: PC-25820Not For Human Use, Lab Use Only.

TP-5801 is a potent, specific inhibitor of Thirty-eight-negative kinase-1 (TNK1) with IC50 of 1.4 nM, inhibits TNK1-transformed cells.

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5 mg	￥2880	In stock
10 mg	￥4580	In stock
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生物&药学活性

TP-5801 is a potent, specific inhibitor of Thirty-eight-negative kinase-1 (TNK1) with IC50 of 1.4 nM, inhibits TNK1-transformed cells.
TP-5801is potent IC50 of 10.5 nM against TNK1 in Nano-BRET analysis.
TP-5801 (300 nM) shows clear selectvity profile against a panel of 371 kinases in vitro, only 7 other kinases were inhibited by more than 90%.
TP-5801 inhibits TNK1-driven cell growth with IC50s of 76.78 and 36.95 nM against Ba/F3 WT TNK1 and AAA mutant cells.
TP-5801 inhibits BCR-ABL-driven and IL-3-driven Ba/F3 cell growth with IC50s of 8.5 and 1.2 μM, respectively.
TP-5801 (10 mg/kg, daily oral administration) significantly reduced tumor burden in NOD/SCID mice were subcutaneously injected with TNK1-AAA driven Ba/F3-luc cells.

物理化学性质&存储条件

分子量	527.47
分子式	C24H31BrN8O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-bromo-N4-(2-(dimethylamino)pyridin-3-yl)-N2-(2-methoxy-5-methyl-4-(4-methylpiperazin-1-yl)phenyl)pyrimidine-2,4-diamine

参考文献

1. Chan TY, et al. Nat Commun. 2021 Sep 9;12(1):5337.

TP-5801 (TP5801)

生物&药学活性

物理化学性质&存储条件

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TP-5801 (TP5801)

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