An inhibitor of tubulin polymerization
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ELR510444

Item No. 17696

Technical Information
Formal Name
N-[5-(5-cyano-2-thienyl)-2-methylphenyl]-4-methyl-benzenesulfonamide
CAS Number
1233948-35-0
Molecular Formula
C19H16N2O2S2
Formula Weight
Purity
≥95%
A crystalline solid
Methyl Acetate: 10 mg/ml
λmax
309 nm
SMILES
CC1=CC=C(S(NC2=C(C)C=CC(C3=CC=C(C#N)S3)=C2)(=O)=O)C=C1
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
InChi Key
GRYXROIHHXHFND-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ELR510444 is an inhibitor of tubulin polymerization (IC50 = 10 μM) that binds to tubulin at the colchicine (Item No. 9000760) binding site.1 It induces microtubule depolymerization in A-10 cells (EC50 = 21 nM). ELR510444 inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest. Oral administration of ELR510444 (3-6 mg/kg) reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner. ELR510444 also inhibits hypoxia-inducible factor 1α (HIF-1α) in RCC4 cells in a concentration-dependent manner.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Risinger, A.L., Westbrook, C.D., Encinas, A., et alELR510444, a novel microtubule disruptor with multiple mechanisms of action. J. Pharmacol. Exp. Ther. 336(3), 652-660 (2011).

    2. Carew, J.S., Esquivel, J.A., II, Espitia, C.M., et alELR510444 inhibits tumor growth and angiogenesis by abrogating HIF activity and disrupting microtubules in renal cell carcinoma. PLoS One 7(1), e31120 (2012).