Specification
Description
HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor against human head and neck squamous cell carcinoma (HNSCC).
Synonyms
HJC0152; HJC 0152; HJC-0152
IUPAC Name
2-(2-Amino-ethoxy)-5-chloro-N-(2-chloro-4-nitrophenyl)benzamide Hydrochloride
Canonical SMILES
O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[H]Cl
InChI
InChI=1S/C15H13Cl2N3O4.ClH/c16-9-1-4-14(24-6-5-18)11(7-9)15(21)19-13-3-2-10(20(22)23)8-12(13)17;/h1-4,7-8H,5-6,18H2,(H,19,21);1H
InChI Key
XRZHLOYBZOONSZ-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
HJC0152 hydrochloride is a signal transducers and activators of transcription 3 (STAT3) inhibitor.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 44.31; H, 3.47; Cl, 26.15; N, 10.33; O, 15.74
HS Tariff Code
2934.99.9001
In Vitro Activity
As shown in Figure Figure1C-E, HJC0152 showed a significant inhibitory effect that was both concentration- and time-dependent. The IC50 values of HJC0152 against A549, H460 and H1299 cells were 5.11, 5.01 and 13.21 μmol/L, respectively (Figure 1F-H). These findings suggest that HJC0152 has a strong cytostatic and cytotoxic effect on NSCLC cells and that NSCLC cells with higher p-STAT3 (Tyr705) levels are more sensitive to HJC0152.
Reference: Cell Prolif. 2020 Mar;53(3):e12777. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7106968/
In Vivo Activity
To determine the anti-tumor effect of HJC0152 in vivo, nude mice were subcutaneously inoculated with MKN45 cells and treated with HJC0152 (7.5 mg/kg) or PBS. As exhibited in Figure 3A-C, the tumor volumes (P<0.001) and tumor weight (P<0.01) were significantly lower in the HJC0152-treated group compared with the control group.
Reference: Cancer Manag Res. 2018 Dec 12;10:6857-6867. https://pubmed.ncbi.nlm.nih.gov/30588091/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).