HJC0416 hydrochloride is a potent and orally activeSTAT3inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breastcancerstudy^[1].

HJC0416 hydrochloride inhibits the proliferation of both ER-positive, and ER-negative (triple negative) breast cancer cells with IC₅₀ values of 1.76 μM and 1.97 μM, respectively. However, it displays a marked antiproliferative effect against pancreatic cancer cell line AsPC1 and Panc-1 with IC₅₀ values of 40 nM and 1.88 μM, respectively^[1].
HJC0416 hydrochloride (1-10 μM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells^[1].
HJC0416 hydrochloride (5 μM; 24 hours) decreases the STAT3 promoter activity by approximately 51%, while stattic (HY-13818) only decreases the STAT3 promoter activity by 39% in MDA-MB-231 cells after transient transfecting with pSTAT3-Luc vector^[1].
HJC0416 hydrochloride (1-10 μM; 12 hours) has a comparable potency in downregulating STAT3 protein production and phosphorylation at Tyr-705 site when compares with Stattic (HY-13818). Additionally, it also induces cleaved caspase-3 and downregulated cyclin D1 levels in MDA-MB-231 cells^[1].

HJC0416 hydrochloride (intraperitoneal injection; 10 mg/kg; 7 days) shows a 67% decrease of tumor volume as compared to the control mice. Similarly, HJC0416 hydrochloride (oral administration; 100 mg/kg; 14 days) also significantly reduces tumor volume at a dose of 100 mg/kg by 46%. The i.p. route appeared to have a better reduction of tumor volume. It is also noteworthy that HJC0416 does not show significant signs of toxicity at a dose of 100 mg/kg^[1].

429.32

C₁₈H₁₈Cl₂N₂O₄S

2415263-08-8

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 1.

  All drugs were dissolved in 50% DMSO with 50% polyethylene glycol for in vivo administration^[1].