1. JAK/STAT Signaling
    Stem Cell/Wnt
    Apoptosis
  2. STAT
    Apoptosis
  3. HJC0416 hydrochloride

HJC0416 hydrochloride 

Cat. No.: HY-12352A
Handling Instructions

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study.

For research use only. We do not sell to patients.

HJC0416 hydrochloride Chemical Structure

HJC0416 hydrochloride Chemical Structure

CAS No. : 2415263-08-8

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Description

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].

IC50 & Target[1]

STAT3

 

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[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].

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 1-10 µM
Incubation Time: 48 hours
Result: Induced cell apoptosis in cancer cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 breast cancer cells
Concentration: 1 µM; 5 µM; 10 µM
Incubation Time: 12 hours
Result: Decreased p-STAT3 phosphorylation expression and cyclin D1 level.
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[1].

Animal Model: Mice with MDA-MB-231 cells[1]
Dosage: 10 mg/kg (i.p.); 100 mg/kg (oral)
Administration: Intraperitoneal injection, 7 days; oral administration, 14 days
Result: Exhibited antitumor effects in the MDA-MB-231 triple-negative breast cancer murine xenograft model.
Molecular Weight

429.32

Formula

C₁₈H₁₈Cl₂N₂O₄S

CAS No.

2415263-08-8

SMILES

O=C(NC1=CC=C(C=CS2(=O)=O)C2=C1)C3=CC(Cl)=CC=C3OCCCN.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
In Vivo:
  • 1.

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

References
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Keywords:

HJC0416HJC 0416HJC-0416STATApoptosistranscription 3?anticancerBreastMCF-7MDA-MB-231PancreaticAsPC1Panc-1StatticInhibitorinhibitorinhibit

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HJC0416 hydrochloride
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