1172133-28-6|HO-3867|CsnPharm

CAS No.: 1172133-28-6

HO-3867 Catalog No. CSN19012

Synonyms: N/A

HO-3867 selectively inhibits the phosphorylation and transcription of STAT3. It is an analog of curcumin.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述HO-3867, a curcumin analogue, is a selective STAT3 inhibitor. It selectively inhibited STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs at 10μM. HO-3867 significantly inhibited BRCA-mutated ovarian cancer cells expressing higher level of Tyrosine-phosphorylated STAT3 (pTyr705) in vitro, in a dose (1-20μM)- and time (12-48h)-dependent manner, with apoptosis shown by elevated levels of cleaved caspase-3, caspase-7 and PARP. Also, treatment with HO-3867 resulted in decreased expression of pTyr705 and its downstream targets cyclin D1, Bcl-2 and surviving in these cells. HO-3867 is a safe STAT3 Inhibitor for it exhibited minimal toxicity toward noncancerous cells and tissues but induced apoptosis in ovarian cancer cells. It inhibited cell migration/invasion and survival of primary human ovarian cancer cells isolated from patient ascites at 10μM post 24h. Administration of HO-3867 at 100ppm could block xenograft tumor growth without toxic side effects in nude mice injected with A2780 cells.
作用机制HO-3867 has high affinity for a pocket located on the DNA-binding domain of the STAT3 and it could interact with both the STAT3 dimer and monomer structures.^[1]
动物研究
剂量
Mice: 20 mg/kg^[3] (i.v.) Rat: 10 mg/kg, 25 mg/kg^[4] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 20 mg/kg^[3] (i.v.) Rat: 10 mg/kg, 25 mg/kg^[4] (i.p.)
给药途径	i.v., i.p.

[1] Rath KS, Naidu SK, et al. HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27.
[2] Tierney BJ, McCann GA, et al. HO-3867, a STAT3 inhibitor induces apoptosis by inactivation of STAT3 activity in BRCA1-mutated ovarian cancer cells. Cancer Biol Ther. 2012 Jul;13(9):766-75.
[3] Madan E, Parker TM, et al. The curcumin analog HO-3867 selectively kills cancer cells by converting mutant p53 protein to transcriptionally active wildtype p53. J Biol Chem. 2018 Mar 23;293(12):4262-4276.
[4] Dayton A, Selvendiran K, et al. Cellular uptake, retention and bioabsorption of HO-3867, a fluorinated curcumin analog with potential antitumor properties. Cancer Biol Ther. 2010 Nov 15;10(10):1027-32.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1526 mL
- 10.7632 mL
- 21.5264 mL
- 5 mM
- 0.4305 mL
- 2.1526 mL
- 4.3053 mL
- 10 mM
- 0.2153 mL
- 1.0763 mL
- 2.1526 mL

技术信息

CAS号

1172133-28-6

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H30F2N2O2

运输

蓝冰

分子量

464.55

别名

N/A

溶解度

DMSO	50.0 mg/mL (107.6 mM)
Water	insoluble

动物实验配方

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HO-3867 Catalog No. CSN19012

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