ELR510444 |
Catalog No.GC16827
One-Click Copy Product Info
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ELR510444 es un nuevo disruptor de microtÚbulos; inhibe la proliferaciÓn de células MDA-MB-231 con IC50 de 30,9 nM; no es un sustrato para el transportador de fÁrmacos de la glicoproteÍna P y retiene la actividad en lÍneas celulares que sobreexpresan βIII-tubulina.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1233948-35-0
Sample solution is provided at 25 µL, 10mM.
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Microtubules are involved in nucleic and cell organization, division of intracellular structure, and intracellular transport, as well as ciliary and flagellar motility. Microtubule-targeting agents are some of the most effective chemotherapeutic drugs used in the clinic today. ELR510444 is a novel microtubule disruptor with multiple mechanisms of action.
In vitro: ELR510444 has potent microtubuledisrupting activity, causing a loss of intracellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 inhibited cell proliferation, inhibited the rate and extent of purified tubulin assembly potently, and displaced colchicine from tubulin, revealing that the drug directly interacts with tubulin at the colchicine-binding site [1].
In vivo: ELR510444 also shows potent antitumor activity in the MDA-MB-231 xenograft model with at least a 2-fold therapeutic window [1].
Clinical trial: Up to now, ELR510444 is still in the preclinical development stage.
Reference:
[1] Risinger AL, Westbrook CD, Encinas A, Mülbaier M, Schultes CM, Wawro S, Lewis JD, Janssen B, Giles FJ, Mooberry SL. ELR510444, a novel microtubule disruptor with multiple mechanisms of action. J Pharmacol Exp Ther. 2011 Mar;336(3):652-60.
| Cas No. | 1233948-35-0 | SDF | |
| Chemical Name | N-(5-(5-cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide | ||
| Canonical SMILES | CC1=CC=C(S(NC2=C(C=CC(C3=CC=C(S3)C#N)=C2)C)(=O)=O)C=C1 | ||
| Formula | C19H16N2O2S2 | M.Wt | 368.47 |
| Solubility | ≥ 11.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7139 mL | 13.5696 mL | 27.1393 mL |
| 5 mM | 542.8 μL | 2.7139 mL | 5.4279 mL |
| 10 mM | 271.4 μL | 1.357 mL | 2.7139 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)