Cat. No.: HY-12352A

HJC0416 hydrochloride

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

Purity: 98.68%
CAS No.: 2415263-08-8
Formula: C₁₈H₁₈Cl₂N₂O₄S
Molecular Weight:429.32

Storage:

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

HJC0416 hydrochloride Chemical Structure

CAS No.: 2415263-08-8

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

STAT3

All STAT Isoforms :

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS No. 2415263-08-8
Appearance Solid
Molecular Weight 429.32
Formula C₁₈H₁₈Cl₂N₂O₄S
Color White to off-white
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

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (1)

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Journal Impact Factor

Cell Mol Gastroenterol Hepatol

Siglec-H-/- Plasmacytoid Dendritic Cells Protects Against Acute Liver Injury by Suppressing IFN-γ/Th1 Response and Promoting IL-21+ CD4 T Cells. [Abstract]

2024 Jun 5:101367. PMID: 38849082

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (232.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3293 mL

11.6463 mL

23.2926 mL

5 mM

0.4659 mL

2.3293 mL

4.6585 mL

10 mM

0.2329 mL

1.1646 mL

2.3293 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Haijun Chen, et al.Discovery of Potent Anticancer Agent HJC0416, an Orally Bioavailable Small Molecule Inhibitor of Signal Transducer and Activator of Transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3293 mL	11.6463 mL	23.2926 mL	58.2316 mL
	5 mM	0.4659 mL	2.3293 mL	4.6585 mL	11.6463 mL
	10 mM	0.2329 mL	1.1646 mL	2.3293 mL	5.8232 mL
	15 mM	0.1553 mL	0.7764 mL	1.5528 mL	3.8821 mL
	20 mM	0.1165 mL	0.5823 mL	1.1646 mL	2.9116 mL
	25 mM	0.0932 mL	0.4659 mL	0.9317 mL	2.3293 mL
	30 mM	0.0776 mL	0.3882 mL	0.7764 mL	1.9411 mL
	40 mM	0.0582 mL	0.2912 mL	0.5823 mL	1.4558 mL
	50 mM	0.0466 mL	0.2329 mL	0.4659 mL	1.1646 mL
	60 mM	0.0388 mL	0.1941 mL	0.3882 mL	0.9705 mL
	80 mM	0.0291 mL	0.1456 mL	0.2912 mL	0.7279 mL
	100 mM	0.0233 mL	0.1165 mL	0.2329 mL	0.5823 mL

Keywords

HJC0416 hydrochloride

1 Cited Publications

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HJC0416 hydrochloride

Apoptosis Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Small Molecule Immuno-Oncology Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) HJC0416 hydrochloride

All STAT Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

HJC0416 hydrochloride Related Classifications

Cat. No.: HY-12352A