| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Vimentin-IN-1 (compound 4e) (0-10 mM; 72 h) is much more potent than FiVe1 (IC50=1.6 μM, HT-1080) at inhibiting HT-1080 fibrosarcoma, with an IC50 value of 44 nM [1]. Phosphorylation of VIM Ser56 is induced by venterin-IN-1 (0.1 μM; 24 hours) [1]. In mouse liver microsomes, ventin-IN-1 (100 μM) is less stable; after 60 minutes of incubation, 0.0% is still present [1]. Samples are taken at 0, 5, 15, 30, 45, and 60 minutes.
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|---|---|
| ln Vivo |
The oral pharmacokinetic properties of Vimentin-IN-1 (Compound 4e) (10 mg/kg; single dose) are superior to those of Five1 [1]. Vimentin-IN-1's pharmacokinetic characteristics in mice [1] The dosage by route (mg/kg) AUC0-last (ng·h/mL) AUC0-inf (ng·h/mL) T1/2 (hour) Tmax (h), Cmax (ng/mL), and Final (h) 4e PO 25 309.78 339.21 4.57 0. 5 18 110.43 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
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HT-1080, RD and MCF-7 Cell Tested Concentrations: 0-10 mM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibition of HT-1080, RD and MCF-7 cells with IC50 of 44 nM, 61 nM and 49 nM respectively. |
| References |
| Molecular Formula |
C19H18CL2N4O
|
|---|---|
| Molecular Weight |
389.278421878815
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| Exact Mass |
388.085
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| CAS # |
2319587-80-7
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| PubChem CID |
156552418
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| Appearance |
Light yellow to orange solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
463
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JWIRSMDIIXNJAU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18Cl2N4O/c1-26-15-10-13(20)9-14(11-15)24-5-7-25(8-6-24)18-12-22-23-19-16(18)3-2-4-17(19)21/h2-4,9-12H,5-8H2,1H3
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| Chemical Name |
8-chloro-4-[4-(3-chloro-5-methoxyphenyl)piperazin-1-yl]cinnoline
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~64.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.42 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. 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 | 2.5688 mL | 12.8442 mL | 25.6885 mL | |
| 5 mM | 0.5138 mL | 2.5688 mL | 5.1377 mL | |
| 10 mM | 0.2569 mL | 1.2844 mL | 2.5688 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.
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