Vimentin-IN-1
Based on 1 Customer Validation
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1.
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- Purity: 99.74%
- CAS No.: 2319587-80-7
- 화학식: C19H18Cl2N4O
- 분자량:389.28
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Bioactive Compound Library Max
HY-L181
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Bioactive Compound Library
HY-L001
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Metabolism/Protease Compound Library
HY-L012
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Ubiquitination Compound Library
HY-L050
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Orally Active Compound Library
HY-L061
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Highly Selective Inhibitors Library
HY-L158
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MCE Bioactive Compound Library
HY-L001V
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Biological Activity
vimentin (VIM)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| GCT | IC50 |
49 nM
Compound: 4e
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Antiproliferative activity against human GCT cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
Antiproliferative activity against human GCT cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
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[PMID: 36001933] |
| HT-1080 | IC50 |
44 nM
Compound: 4e
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Antiproliferative activity against human HT-1080 cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
Antiproliferative activity against human HT-1080 cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
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[PMID: 36001933] |
| MCF7 | IC50 |
11150 nM
Compound: 4e
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
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[PMID: 36001933] |
| RD | IC50 |
61 nM
Compound: 4e
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Antiproliferative activity against human RD cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
Antiproliferative activity against human RD cells assessed as inhibition of cell growth measured after 72 hrs by Celltiter-glo proliferation assay
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[PMID: 36001933] |
Vimentin-IN-1 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC50=1.6 μM, HT-1080)[1].
Vimentin-IN-1 (0.1 μM; 24 h) induces phosphorylation of VIM at Ser56[1].
Vimentin-IN-1 (100 μM; sampled at 0, 5, 15, 30, 45, and 60 min) exhibits poor stability with 0.0% remaining after 60 min of incubation in mouse liver microsome[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-1080, RD, and MCF-7 cells
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Concentration:0-10 mM
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Incubation Time:72 hours
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Result:Inhibited HT-1080, RD, and MCF-7 cells with IC50s of 44 nM, 61 nM, and 49 nM, respectively.
Pharmacokinetic properties of Vimentin-IN-1 in mice[1]
| Route | Dose (mg/kg) | AUC0-last (ng·h/mL) | AUC0-inf (ng·h/mL) | T1/2 (h) | Tmax (h) | Tlast (h) | Cmax (ng/mL) | |
| 4e | PO | 10 | 371.33 | 534.33 | 4.68 | 0.67 | 8 | 154.67 |
| 4e | IP | 1 | 208.33 | 211.33 | 0.59 | 0.25 | 4 | 197.00 |
| Five1 | PO | 25 | 309.78 | 339.21 | 4.57 | 0.5 | 18 | 110.43 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2319587-80-7
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Appearance Solid
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분자량 389.28
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화학식 C19H18Cl2N4O
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Color Light yellow to orange
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SMILES
COC1=CC(Cl)=CC(N2CCN(C3=C4C=CC=C(Cl)C4=NN=C3)CC2)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 25 mg/mL (64.22 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 (6.42 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
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.
순도&문서
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Data Sheet (275 KB)
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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)
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Handling Instructions (2659 KB)
References
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 | 2.5688 mL | 12.8442 mL | 25.6885 mL | 64.2211 mL |
| 5 mM | 0.5138 mL | 2.5688 mL | 5.1377 mL | 12.8442 mL | |
| 10 mM | 0.2569 mL | 1.2844 mL | 2.5688 mL | 6.4221 mL | |
| 15 mM | 0.1713 mL | 0.8563 mL | 1.7126 mL | 4.2814 mL | |
| 20 mM | 0.1284 mL | 0.6422 mL | 1.2844 mL | 3.2111 mL | |
| 25 mM | 0.1028 mL | 0.5138 mL | 1.0275 mL | 2.5688 mL | |
| 30 mM | 0.0856 mL | 0.4281 mL | 0.8563 mL | 2.1407 mL | |
| 40 mM | 0.0642 mL | 0.3211 mL | 0.6422 mL | 1.6055 mL | |
| 50 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2844 mL | |
| 60 mM | 0.0428 mL | 0.2141 mL | 0.4281 mL | 1.0704 mL |
Vimentin-IN-1 Related Classifications
HY-151424 Related Classifications
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