ELR510444
ELR510444 is a potent microtube disruptor with potential anticancer activity. ELR510444 has potent microtubule-disrupting activity, causing a loss of cellular microtubules and the formation of aberrant mitotic spindles and leading to mitotic arrest and apoptosis of cancer cells. ELR510444 potently inhibited cell proliferation with an IC(50) value of 30.9 nM in MDA-MB-231 cells, inhibited the rate and extent of purified tubulin assembly, and displaced colchicine from tubulin, indicating that the drug directly interacts with tubulin at the colchicine-binding site.
1: Carew JS, Esquivel JA 2nd, Espitia CM, Schultes CM, Mülbaier M, Lewis JD, Janssen B, Giles FJ, Nawrocki ST. ELR510444 inhibits tumor growth and angiogenesis by abrogating HIF activity and disrupting microtubules in renal cell carcinoma. PLoS One. 2012;7(1):e31120. doi: 10.1371/journal.pone.0031120. Epub 2012 Jan 25. PubMed PMID: 22295124; PubMed Central PMCID: PMC3266297.
2: 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. doi: 10.1124/jpet.110.175331. Epub 2010 Dec 9. PubMed PMID: 21148249; PubMed Central PMCID: PMC3061540.
2: 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. doi: 10.1124/jpet.110.175331. Epub 2010 Dec 9. PubMed PMID: 21148249; PubMed Central PMCID: PMC3061540.
| Chemical | |
|---|---|
| CAS Num | 1233948-35-0 |
| Chemical Formula | C19H16N2O2S2 |
| Molecular Weight | 368.47 |
| IUPAC Chemical Name | N-(5-(5-cyanothiophen-2-yl)-2-methylphenyl)-4-methylbenzenesulfonamide |
| Exact Mass | 368.06532 |
| Elemental Analysis | C, 61.93; H, 4.38; N, 7.60; O, 8.68; S, 17.40 |
| Synonym | ELR510444; ELR-510444; ELR 510444. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=S(C1=CC=C(C)C=C1)(NC2=CC(C3=CC=C(C#N)S3)=CC=C2C)=O |
| Biological | |
| Targets and Effects | N/A |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Yellow solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >2 years if stored properly |
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