HJC0416,2415263-08-8

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HJC0416 hydrochloride

CAS No. : 2415263-08-8

MCE 国际站：HJC0416 hydrochloride

产品活性：HJC0416 hydrochloride 是一种有效的口服活性 STAT3 抑制剂，具有比 Stattic (HY-13818) 更强的抗癌活性。HJC0416 hydrochloride 是一种很有前途的抗乳腺癌试剂。

研究领域：JAK/STAT Signaling  |  Stem Cell/Wnt  |  Apoptosis

作用靶点：STAT  |  Apoptosis

In Vitro: 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.
HJC0416 hydrochloride (1-10 µM; 48 hours) inhibits cell growth and induced apoptosis accompanying cellular morphological changes in MDA-MB-231 breast cancer cells.
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.
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.

In Vivo: 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.

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