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Purity: ≥98%
ELR-510444 is a novel and potent inhibitor of microtubule polymeirzation (also called microtubule disruptor or mitotic inhibitor) with potential antivascular effects and in vivo antitumor efficacy, it can cause a loss of cellular microtubules and the formation of aberrant mitotic spindles which lead to mitotic arrest and apoptosis of cancer cells. Additionally, in the MDA-MB-231 xenograft model, ELR510444 exhibits strong antitumor activity with a minimum 2-fold therapeutic window. Research on tumor endothelial cells demonstrates that ELR510444, at a low concentration (30 nM), quickly changes the shape of endothelial cells; this effect is comparable to that of combretastatin A4, a vascular disrupting agent.
| Targets |
Microtubule
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
ELR510444 has potent microtubule-disrupting action, which results in aberrant mitotic spindle formation, loss of cellular microtubules, mitotic arrest, and cancer cell apoptosis.
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| Cell Assay |
On glass coverslips, 2H-11 cells are plated and given 24 hours to adhere and proliferate. Following the addition of drugs for one hour, cells are permeabilized with Triton X-100 and fixed with paraformaldehyde. Phalloidin conjugated with tetramethylrhodamine B isothiocyanate and DAPI are used to stain F-actin and DNA, respectively.
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| Animal Protocol |
BALB/c nude mice
3, 6, and 12.5 mg/kg s.c. |
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| References |
| Molecular Formula |
C19H16N2O2S2
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| Molecular Weight |
368.47
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| Exact Mass |
368.07
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| Elemental Analysis |
C, 61.93; H, 4.38; N, 7.60; O, 8.68; S, 17.40
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| CAS # |
1233948-35-0
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| Related CAS # |
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| Appearance |
Yellow solid powder
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| SMILES |
CC1=CC=C(C=C1)S(=O)(=O)NC2=C(C=CC(=C2)C3=CC=C(S3)C#N)C
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| InChi Key |
GRYXROIHHXHFND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16N2O2S2/c1-13-3-8-17(9-4-13)25(22,23)21-18-11-15(6-5-14(18)2)19-10-7-16(12-20)24-19/h3-11,21H,1-2H3
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| Chemical Name |
N-[5-(5-cyanothiophen-2-yl)-2-methylphenyl]-4-methylbenzenesulfonamide
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| Synonyms |
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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 |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7139 mL | 13.5696 mL | 27.1393 mL | |
| 5 mM | 0.5428 mL | 2.7139 mL | 5.4279 mL | |
| 10 mM | 0.2714 mL | 1.3570 mL | 2.7139 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.
Products are for research use only; We do not sell to patients
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