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| 10mg |
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Purity: ≥98%
HO-3867 (HO3867; HO 3867), an analog of curcumin, is a novel, selective and potent STAT3 inhibitor with potential antitumor activity. HO-3867 selectively inhibited STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. O-3867 may be useful to treat ovarian cancer and other solid tumors where STAT3 is commonly upregulated. HO-3867 exhibited minimal toxicity toward noncancerous cells and tissues but induced apoptosis in ovarian cancer cells. Pharmacologic analysis revealed greater bioabsorption and bioavailability of the active (cytotoxic) metabolites in cancer cells compared with normal cells.
| ln Vitro |
While HO-3867 causes ovarian cancer cells to undergo apoptosis, it is not harmful to non-cancerous cells or organs. Through the inhibition of STAT3 phosphorylation, HO-3867 prevents cell migration, invasion, and survival [1]. Following treatment with HO-3867, BRCA-mutant ovarian cancer cells displayed a notable degree of apoptosis along with elevated levels of cleaved caspase-3, caspase-7, and PARP [2]. At a concentration of 2 μMol/L, HO-3867 demonstrates strong anti-tumor activity in PANC-1 and BXPC-3 cells. Reactive oxygen species (ROS) production in human pancreatic cancer cell lines was reported to be considerably enhanced by HO-3867 treatment, which in turn induced PANC-1 and BXPC-3 cells [3].
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| ln Vivo |
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| Animal Protocol |
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| References |
[1]. Rath KS et al. HO-3867, a safe STAT3 inhibitor, is selectively cytotoxic to ovarian cancer. Cancer Res. 2014 Apr 15;74(8):2316-27.
[2]. Hu Y, et al. A novel STAT3 inhibitor HO-3867 induces cell apoptosis by reactive oxygen species-dependent endoplasmic reticulum stress in human pancreatic cancer cells. Anticancer Drugs. 2017 Apr;28(4):392-400. [3]. Tierney BJ 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 |
| Molecular Formula |
C28H30F2N2O2
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| Molecular Weight |
464.55
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| CAS # |
1172133-28-6
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| Related CAS # |
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| SMILES |
FC1C([H])=C([H])C(=C([H])C=1[H])/C(/[H])=C1/C(/C(=C(\[H])/C2C([H])=C([H])C(=C([H])C=2[H])F)/C([H])([H])N(C/1([H])[H])C([H])([H])C1=C([H])C(C([H])([H])[H])(C([H])([H])[H])N(C1(C([H])([H])[H])C([H])([H])[H])O[H])=O
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| InChi Key |
PWZQFTQMMAIRRM-JFMUQQRKSA-N
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| InChi Code |
InChI=1S/C28H30F2N2O2/c1-27(2)15-23(28(3,4)32(27)34)18-31-16-21(13-19-5-9-24(29)10-6-19)26(33)22(17-31)14-20-7-11-25(30)12-8-20/h5-15,34H,16-18H2,1-4H3/b21-13+,22-14+
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| Chemical Name |
(3E,5E)-3,5-bis(4-fluorobenzylidene)-1-((1-hydroxy-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)methyl)piperidin-4-one
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1526 mL | 10.7631 mL | 21.5262 mL | |
| 5 mM | 0.4305 mL | 2.1526 mL | 4.3052 mL | |
| 10 mM | 0.2153 mL | 1.0763 mL | 2.1526 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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