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Chemical Structure| 1420290-88-5 Chemical Structure| 1420290-88-5

Structure of HJC0152 free base
CAS No.: 1420290-88-5

Chemical Structure| 1420290-88-5

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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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Product Details of HJC0152 free base

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

Safety of HJC0152 free base

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

Related Pathways of HJC0152 free base

JAK-STAT

Isoform Comparison

Biological Activity

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

Protocol

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

 

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