Structure of HJC0152 free base
CAS No.: 1420290-88-5
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
HJC0152 is an effective STAT3 inhibitor with oral activity that inhibits cell cycle progression, induces apoptosis, and significantly suppresses the growth of MDA-MB-231 xenograft tumors in mice, demonstrating antitumor activity and suitability for research on STAT3-related cancers.
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| CAS No. : | 1420290-88-5 |
| Formula : | C15H13Cl2N3O4 |
| M.W : | 370.19 |
| SMILES Code : | O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN |
| MDL No. : | MFCD31704937 |
| GHS Pictogram: |
|
| Signal Word: | Warning |
| Hazard Statements: | H302-H315-H319 |
| Precautionary Statements: | P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330 |
In Vitro:
|
Cell Line
|
Concentration | Treated Time | Description | References |
| H1299 | 1.25, 2.5, 5, 10, 20 μmol/L | 24, 48, 72 hours | HJC0152 significantly inhibited NSCLC cell proliferation with an IC50 value of 13.21 μmol/L (H1299). | Cell Prolif. 2020 Mar;53(3):e12777 |
| H460 | 1.25, 2.5, 5, 10, 20 μmol/L | 24, 48, 72 hours | HJC0152 significantly inhibited NSCLC cell proliferation with an IC50 value of 5.01 μmol/L (H460). | Cell Prolif. 2020 Mar;53(3):e12777 |
| A549 | 1.25, 2.5, 5, 10, 20 μmol/L | 24, 48, 72 hours | HJC0152 significantly inhibited NSCLC cell proliferation with an IC50 value of 5.11 μmol/L (A549). | Cell Prolif. 2020 Mar;53(3):e12777 |
| CAL27 cells | 1 μM | 24 hours | Inhibited cell proliferation, migration and invasion, induced apoptosis | Mol Cancer Ther. 2017 Apr;16(4):578-590 |
| SCC25 cells | 2 μM | 24 hours | Inhibited cell proliferation, migration and invasion, induced apoptosis | Mol Cancer Ther. 2017 Apr;16(4):578-590 |
| 266-6 cells | 10 µM | 48 hours | Inhibits STAT3 activity, rescues p-STAT1 nuclear translocation and enhances ISG expression | Int J Mol Sci. 2024 Aug 19;25(16):9007 |
| Human pulmonary artery endothelial cells (hPAECs) | 1 μM | 48 hours | To investigate the effect of SERCA2a overexpression and STAT3 inhibitor HJC0152 on BMPR2 expression in hPAECs, results showed that STAT3i potentiated SERCA2a-induced BMPR2 expression. | Int J Mol Sci. 2021 Aug 24;22(17):9105 |
| Human pulmonary artery smooth muscle cells (hPASMCs) | 1 μM | 48 hours | To evaluate the effect of STAT3 inhibitor HJC0152 on BMPR2 expression in hPASMCs, results showed that SERCA2a overexpression upregulated BMPR2 expression by inhibiting STAT3 activity. | Int J Mol Sci. 2021 Aug 24;22(17):9105 |
| HGC-27 cells | 0, 5, 10, 20 µM | 0, 24, 48, 72 hours | To evaluate the effect of HJC0152 on cell growth, results showed that HJC0152 only inhibited the growth of HGC-27 cells at relatively high concentrations | Cancer Manag Res. 2018 Dec 12;10:6857-6867 |
| MKN45 cells | 0, 5, 10, 20 µM | 0, 24, 48, 72 hours | To evaluate the effect of HJC0152 on cell growth, results showed that HJC0152 significantly inhibited the growth of MKN45 cells | Cancer Manag Res. 2018 Dec 12;10:6857-6867 |
| AGS cells | 0, 5, 10, 20 µM | 0, 24, 48, 72 hours | To evaluate the effect of HJC0152 on cell growth, results showed that HJC0152 significantly inhibited the growth of AGS cells | Cancer Manag Res. 2018 Dec 12;10:6857-6867 |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| BALB/c nude mice | A549 NSCLC xenograft model | Oral | 7.5 mg/kg | Once daily for 30 days | HJC0152 significantly inhibited the growth of A549 xenograft tumours, extending the tumour volume doubling time from 2.03 days to 4.62 days. | Cell Prolif. 2020 Mar;53(3):e12777 |
| BALB/c-nu mice | SCC25-derived orthotopic tongue tumor model | Intraperitoneal injection | 7.5 mg/kg | Daily administration for 28 days | Significantly inhibited tumor growth and invasion | Mol Cancer Ther. 2017 Apr;16(4):578-590 |
| C57BL/6 mice | CVB3-induced acute pancreatitis and myocarditis model | Intraperitoneal injection | 12.5 mg/kg | Once 24 hours before and once 24 hours after infection | Alleviates viral-induced pancreatitis and myocarditis pathology by increasing IFNβ and ISG expression to reduce viral load | Int J Mol Sci. 2024 Aug 19;25(16):9007 |
| Rats | Severe PAH model induced by unilateral left pneumonectomy combined with monocrotaline (PNT/MCT) | Intraperitoneal injection | 7.5 mg/kg | Single injection, lasting 4 weeks | To evaluate the therapeutic effect of STAT3 inhibitor HJC0152 combined with AAV1.hSERCA2a in the PAH model, results showed that combination therapy significantly reduced pulmonary artery pressure and vascular remodeling, and improved right ventricular function. | Int J Mol Sci. 2021 Aug 24;22(17):9105 |
| Nude mice | MDA-MB-231 xenograft model | Intraperitoneal injection and oral | 7.5 mg/kg (ip), 25 mg/kg (po) | Evaluate the inhibitory effect of HJC0152 on the growth of MDA-MB-231 xenograft tumors | Am J Cancer Res. 2019 Apr 1;9(4):699-713 | |
| Nude mice | MDA-MB-231 xenograft model | Intraperitoneal injection and oral | 7.5 mg/kg (ip), 25 mg/kg (po) | Evaluate the inhibitory effect of HJC0152 on the growth of MDA-MB-231 xenograft tumors | ACS Med Chem Lett. 2013 Feb 14;4(2):180-185 | |
| BALB/c nude mice | MKN45 subcutaneous xenograft model | Intraperitoneal injection | 7.5 mg/kg | Twice weekly for 21 days | To evaluate the anti-tumor effect of HJC0152 in vivo, results showed that HJC0152 significantly inhibited tumor growth | Cancer Manag Res. 2018 Dec 12;10:6857-6867 |
| Bio Calculators | ||||
| Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.70mL 0.54mL 0.27mL |
13.51mL 2.70mL 1.35mL |
27.01mL 5.40mL 2.70mL |
|
Tags: HJC0152 | HJC 0152 | HJC-0152 | STAT | Apoptosis | STAT3 | Niclosamide derivatives | xenograft | inhibitor | 1420290-88-5 |
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