2. Metabolic Enzyme/Protease
  3. Proteasome
  4. Vimentin-IN-1

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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Vimentin-IN-1 Chemical Structure

Vimentin-IN-1 Chemical Structure

CAS No. : 2319587-80-7

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Customer Review

Based on 1 publication(s) in Google Scholar

Vimentin-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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[1].

IC50 & Target

vimentin (VIM)[1]
In Vitro

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.

Vimentin-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: HT-1080, RD, and MCF-7 cells
Concentration: 0-10 mM
Incubation Time: 72 hours
Result: Inhibited HT-1080, RD, and MCF-7 cells with IC50s of 44 nM, 61 nM, and 49 nM, respectively.
In Vivo

Vimentin-IN-1 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1[1].
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.
Molecular Weight

389.28

Formula

C19H18Cl2N4O
CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

COC1=CC(Cl)=CC(N2CCN(C3=C4C=CC=C(Cl)C4=NN=C3)CC2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5688 mL 12.8442 mL 25.6885 mL
5 mM 0.5138 mL 2.5688 mL 5.1377 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
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
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Vimentin-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vimentin-IN-12319587-80-7ProteasomeEpithelial-mesenchymal transitionEMTpharmacokinetic?vimentinVIMmultinucleationhyperphosphorylationmitosis disruptionVIM-expressing mesenchymal cell lineHT-1080MCF-7Inhibitorinhibitorinhibit

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