Tarloxotinib | pan-HER inhibitor | Probechem Biochemicals

Chemical Structure : Tarloxotinib

CAS No.: 1636180-98-7

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Tarloxotinib (TH-4000, TH4000)

货号: PC-25509Not For Human Use, Lab Use Only.

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5 mg	￥2480	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

Tarloxotinib (TH-4000) is a hypoxia-activated pan-HER inhibitor, generates the active form TH-4000Effector (TH-4000E) under hypoxic condition, TH-4000E selectively inhibits EGFR, HER2 and HER4 with IC50 of <1 nM.
TH-4000E has a highly selective inhibitory effect on HER2+ breast cancer cells, shows IC50 of 8.84 nM, 13.14 nM, 108.92 nM and 126.20 nM for HER2+ breast cancer cells BT-474, SK-BR-3, HCC-1954 and JIMT-1 respectively.
TH-4000E showed highest selectivity to EGFR, HER2 and HER4 among 217 kinases, with IC50 of <1 nM.
TH-4000E inhibits phosphorylation of HER family proteins in HER2+ breast cancer cells.
TH-4000E induces cellular apoptosis in HER2+ breast cancer cells, through a ROS-dependent manner.
Tarloxotinib (TH-4000) (50 mg/kg per week by intraperitoneal injection) inhibited tumor growth in a xenograft model.

物理化学性质&存储条件

分子量	681.77
分子式	C24H24Br2ClN9O3
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	(E)-4-((4-((3-Bromo-4-chlorophenyl)amino)pyrido[3,4-d]pyrimidin-6-yl)amino)-N,N-dimethyl-N-((1-methyl-4-nitro-1H-imidazol-5-yl)methyl)-4-oxobut-2-en-1-aminium bromide

参考文献

1. Xinyi Shao, et al. Arch Toxicol. 2024 Mar;98(3):865-881.

Tarloxotinib (TH-4000, TH4000)

生物&药学活性

物理化学性质&存储条件

参考文献

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Tarloxotinib (TH-4000, TH4000)

生物&药学活性

物理化学性质&存储条件

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