HO-3867

HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.

Product information

CAS Number: 1172133-28-6

Molecular Weight: 464.55

Formula: C28H30F2N2O2

Chemical Name: (3E, 5E)-3, 5-bis[(4-fluorophenyl)methylidene]-1-[(1-hydroxy-2, 2, 5, 5-tetramethyl-2, 5-dihydro-1H-pyrrol-3-yl)methyl]piperidin-4-one

Smiles: CC1(C)C=C(CN2C/C(=C\C3C=CC(F)=CC=3)/C(=O)/C(/C2)=C/C2C=CC(F)=CC=2)C(C)(C)N1O

InChiKey: PWZQFTQMMAIRRM-JFMUQQRKSA-N

InChi: 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+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 32 mg/mL (68.88 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

HO-3867 exhibit minimal toxicity toward noncancerous cells and tissues but induce apoptosis in ovarian cancer cells. HO-3867 inhibit cell migration/invasion and survival by inhibiting STAT3 phosphorylation. BRCA-mutated ovarian cancer cells treated with HO-3867 exhibited a significant degree of apoptosis with elevated levels of cleaved caspase-3, caspase-7 and PARP. HO-3867 shows good antitumor activity at the concentration of 2 μmol/L in PANC-1 and BXPC-3 cells. Importantly, it is also found that HO-3867 treatment significantly induced reactive oxygen species (ROS) production in human pancreatic cancer cell lines, inducing PANC-1 and BXPC-3 cells.

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.

Products are for research use only. Not for human use.