HJ445A
Based on 1 Customer Validation
HJ445A is an orally active myoferlin (MYOF) inhibitor with a Kd value of 0.17 μM against human targets. HJ445A directly binds to the MYOF-C2D domain to stabilize the MYOF protein, thereby regulating vesicle trafficking, cell proliferation, colony formation, migration and apoptosis processes in cancer cells, and exhibits anti-tumor efficacy. HJ445A can be used in gastric cancer-related research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.02%
- No. CAS: 3032441-59-8
- Fòrmula: C24H27N7O2
- Peso molecular:445.52
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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Myoferlin |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| AGS | IC50 |
0.46 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human AGS cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human AGS cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| BGC-823 | IC50 |
0.29 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human BGC-823 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human BGC-823 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| BXPC-3 | IC50 |
0.13 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human BXPC-3 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human BXPC-3 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| CWR22R | IC50 |
>10 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human 22Rv1 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human 22Rv1 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| DU-145 | IC50 |
>10 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human DU-145 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human DU-145 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| ES-2 | IC50 |
0.28 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human ES2 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human ES2 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| MGC-803 | IC50 |
0.16 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human MGC-803 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| MGC-803 | IC50 |
60 nM
Compound: 2i; HJ445A
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Antiinvasive activity against human MGC-803 cells incubated for 24 hrs by crystal violet staining based inverted microscopic analysis
Antiinvasive activity against human MGC-803 cells incubated for 24 hrs by crystal violet staining based inverted microscopic analysis
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[PMID: 38054798] |
| MKN-45 | IC50 |
0.14 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human MKN-45 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human MKN-45 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| SGC-7901 | IC50 |
0.44 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human SGC-7901 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human SGC-7901 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
| SK-HEP1 | IC50 |
0.75 μM
Compound: 2i; HJ445A
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Antiproliferative activity against human SK-HEP1 cells incubated for 48 hrs by SRB assay
Antiproliferative activity against human SK-HEP1 cells incubated for 48 hrs by SRB assay
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[PMID: 38054798] |
HJ445A slightly inhibits select CYP450 enzymes with micromolar IC50 values in in vitro[1].
HJ445A (48 h) potently inhibits the proliferation of MGC803 and MKN45 human gastric cancer cells with IC50 values of 0.16 μM and 0.14 μM, respectively[2].
HJ445A (50-100 μM; 1 h) directly binds to MYOF in MKN45 human gastric cancer cells[2].
HJ445A (0.156-10 μM; association time 80 s, dissociation time 160 s) binds directly and reversibly to the purified MYOF-C2D domain with a high affinity KD of 0.17 μM[2].
HJ445A (50-100 nM; 10 days) represses colony formation of MKN45 human gastric cancer cells in a concentration-dependent manner at 50 nM and 100 nM, which correlates with downregulation of p-AKT[2].
HJ445A (62.5-250 nM; 24 h) inhibits migration of MGC803 human gastric cancer cells[2].
HJ445A (100-400 nM) reverses the EMT process in MKN45 human gastric cancer cells in vitro in a concentration-dependent manner, as shown by upregulated E-cadherin and downregulated N-cadherin and Vimentin[2].
HJ445A (0.1-0.8 μM; 48 h) induces apoptosis of MKN45 human gastric cancer cells in a dose-dependent manner[2].
HJ445A weakly inhibits major human CYP450 isozymes, with IC50 values of 14.7 μM for CYP 2C9, 18.8 μM for CYP 2C19, 35.1 μM for CYP 3A4, and >50.0 μM for CYP 1A2 and CYP 2D6[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human gastric cancer cell line MKN45
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Concentration:50 nM, 100 nM
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Incubation Time:10 days
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Result:Inhibited colony formation of MKN45 cells in a concentration-dependent manner, with significant reduction at 50 nM and 100 nM.
Downregulated phosphorylated AKT (p-AKT) levels in a concentration-dependent manner.
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Cell Line:human gastric cancer cell line MGC803
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Concentration:62.5 nM, 125 nM, 250 nM
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Incubation Time:24 h
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Result:Inhibited migration of MGC803 cells in a concentration-dependent manner.
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Cell Line:human gastric cancer cell line MKN45
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Concentration:0.1 μM, 0.2 μM, 0.4 μM, 0.8 μM
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Incubation Time:48 h
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Result:Induced apoptosis of MKN45 cells in a dose-dependent manner, with apoptosis rates of 3.4%, 5.7%, 50.2%, and 54.0% at 0.1, 0.2, 0.4, and 0.8 μM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-8 weeks old)[2]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.p.; daily
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Result:Achieved a tumor growth inhibition (TGI) of 55.1%.
Achieved a TGI of 68.5%.
Showed no significant difference in mouse body weight compared with the control group.
Caused no visible tissue damage in the lung, liver, heart, kidney, or spleen at 30 mg/kg/day.
Chemical Information
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No. CAS 3032441-59-8
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Appearance Solid
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Peso molecular 445.52
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Fòrmula C24H27N7O2
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Color White to off-white
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SMILES
CCC1=NN(C2=CC=CC(C(NCCCCN3N=CC=N3)=O)=C2)C(C4=CC=C(C=C4)OC)=N1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (224.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (5.61 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.61 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Gullo C, et al. Focal adhesion assembly and cell migration require myoferlin in PDAC cell lines. Sci Rep. 2025 Nov 28;15(1):42797. [Content Brief]
[2]. Gu H, et al. Discovery of a Highly Potent and Selective MYOF Inhibitor with Improved Water Solubility for the Treatment of Gastric Cancer. J Med Chem. 2023 Dec 28;66(24):16917-16938. [Content Brief]
Complete Stock Solution Preparation Table
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2446 mL | 11.2228 mL | 22.4457 mL | 56.1142 mL |
| 5 mM | 0.4489 mL | 2.2446 mL | 4.4891 mL | 11.2228 mL | |
| 10 mM | 0.2245 mL | 1.1223 mL | 2.2446 mL | 5.6114 mL | |
| 15 mM | 0.1496 mL | 0.7482 mL | 1.4964 mL | 3.7409 mL | |
| 20 mM | 0.1122 mL | 0.5611 mL | 1.1223 mL | 2.8057 mL | |
| 25 mM | 0.0898 mL | 0.4489 mL | 0.8978 mL | 2.2446 mL | |
| 30 mM | 0.0748 mL | 0.3741 mL | 0.7482 mL | 1.8705 mL | |
| 40 mM | 0.0561 mL | 0.2806 mL | 0.5611 mL | 1.4029 mL | |
| 50 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1223 mL | |
| 60 mM | 0.0374 mL | 0.1870 mL | 0.3741 mL | 0.9352 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2806 mL | 0.7014 mL | |
| 100 mM | 0.0224 mL | 0.1122 mL | 0.2245 mL | 0.5611 mL |
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