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Purity: ≥98%
HJC0152 hydrochloride is a novel, orally bioavailable and potent inhibitor of the signal transducers and activators of transcription 3 (STAT3). It has potential application for treating human head and neck squamous cell carcinoma (HNSCC). HJC0152 has been demonstrated to significantly suppress MDA-MB-231 xenograft tumor growth in vivo (i.p. & p.o.), indicating its great potential as efficacious and orally bioavailable therapeutics for human cancers. HJC0152 was designed and developed based on niclosamide which has been identified to potently inhibit the activation, nuclear translocation, and transactivation of STAT3 but with pharmacokinetics such as poor aqueous solubility and bioavailability of niclosamide. HJC0152 has improved pharmacokinetic profiles.
| ln Vitro |
At concentrations of 1, 5, and 10 μM, HJC0152 (compound 11) dramatically reduced cell proliferation and induced apoptosis along with alterations in cell morphology. The findings demonstrated that treatment with 10 μM HJC0152 decreased STAT3 promoter activity in MDA-MB-231 cells by roughly 32% in comparison to the control, and that STAT3 promoter activity was further reduced by 62% upon increasing the dose of HJC0152 to 20 μM. Following HJC0152 treatment, total STAT3 fell. In MDA-MB-231 cells, HJC0152 downregulates cyclin D1 and induces cleaved caspase-3 [1].
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| ln Vivo |
Compound 11 (HJC0152; 7.5, 25 mg/kg, ip) prevents transplanted tumors in mice from growing. Furthermore, HJC0152 did not exhibit any overt toxicity at a 75 mg/kg dose [1].
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| References |
[1]. Chen H, et al. Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents. ACS Med Chem Lett. 2013 Feb 14;4(2):180-185
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| Molecular Formula |
C15H14CL3N3O4
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| Molecular Weight |
406.64
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| CAS # |
1420290-99-8
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| Related CAS # |
HJC0152 free base;1420290-88-5
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| SMILES |
O=C(NC1=CC=C([N+]([O-])=O)C=C1Cl)C2=CC(Cl)=CC=C2OCCN.[H]Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 10 mg/mL (24.59 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4592 mL | 12.2959 mL | 24.5918 mL | |
| 5 mM | 0.4918 mL | 2.4592 mL | 4.9184 mL | |
| 10 mM | 0.2459 mL | 1.2296 mL | 2.4592 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
In vivo efficacy of compound11(HJC0152) in inhibiting growth of xenograft tumors (breast cancer MDA-MB-231) in mice. (A) ip and (B) po.ACS Med Chem Lett.2013 Feb 14;4(2):180-185. |
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(A) HJC0152 inhibited the STAT3-mediated luciferase reporter activity in MDA-MB-231 cells. (B) Proliferation of MDA-MB-231 cells treated with HJC0152 and niclosamide for 24 h.ACS Med Chem Lett.2013 Feb 14;4(2):180-185. |
(A) Western blot analysis of biochemical markers for apoptosis induction and inhibition of STAT3 activity by HJC0152 in the MDA-MB-231 cell line. (B) Densitometric analysis of three independent experiments for the expression level of total STAT3, phospho-STAT3, cyclin D1, and cleaved caspase 3.ACS Med Chem Lett.2013 Feb 14;4(2):180-185. |
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