TR-107 (TR107)

Chemical Structure : TR-107

CAS No.: 2485052-87-5

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货号: PC-49211Not For Human Use, Lab Use Only.

规格	价格	库存
10 mg	￥880	In stock
25 mg	￥1380	In stock
50 mg	￥2180	In stock
100 mg		Get quote

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生物&药学活性

TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.
TR-107 dose-dependent increases ClpP activity, inhibits breast cancer cell MDA-MB-231 and SUM159 growth (IC50=23 and 12 nM) in a ClpP-dependent manner, without a significant increase in apoptosis.
TR-107 showed significantly enhanced potency of cell growth inhibition in the MDA-MB-231 and SUM159 cell models compared with ONC201 and ONC206.
TR-107 (100 nM, 6-24 h) induces time- and dose-dependent reduction of multiple mitochondrial proteins (TUFM and TFAM, aconitase (ACO2) and isocitrate dehydrogenase (IDH2), and succinate dehydrogenase A (SDHA) and complex I subunit NDUFS3).
TR-107 reduces mitochondrial metabolic functions and inhibits OXPHOS in MDA-MB-231 cells.
TR-107 (4-8 mg/kg, p.o.) prevents tumor growth in MDA-MB-231 xenograft model.

物理化学性质&存储条件

分子量	390.871
分子式	C22H19ClN4O
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	3-((3-(4-chlorobenzyl)-4-oxo-3,5,7,8-tetrahydropyrido[4,3-d]pyrimidin-6(4H)-yl)methyl)benzonitrile

参考文献

1. Fennell EMJ, et al. Pharmacol Res Perspect. 2022 Aug;10(4):e00993.

TR-107 (TR107)

生物&药学活性

物理化学性质&存储条件

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TR-107 (TR107)

生物&药学活性

物理化学性质&存储条件

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