NVP-TAE684 is an inhibitor of anaplastic lymphoma kinase (ALK), c-Fes, and LRRK2 that exhibits anticancer chemotherapeutic activity. NVP-TAE684 induces apoptosis in and inhibits growth of diffuse large B-cell lymphoma cells; in animal models, it induces tumor regression. NVP-TAE684 also induces cell cycle arrest and apoptosis in animal models of anaplastic large-cell lymphoma, preventing lymphomagenesis and inducing regression.
| Cas No. | 761439-42-3 |
|---|---|
| Purity | ≥98% |
| Formula | C30H40ClN7O3S |
| Formula Wt. | 614.21 |
| IUPAC Name | 5-Chloro-N4-[2-(isopropylsulfonyl)phenyl]-N2-{2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl}-2,4-pyrimidinediamine |
| Synonym | TAE684 |
| Appearance | Yellow to pale yellow powder |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| Info Sheet | N8760 Info Sheet PDF |
|---|
Hellwig S, Miduturu CV, Kanda S, et al. Small-molecule inhibitors of the c-Fes protein-tyrosine kinase. Chem Biol. 2012 Apr 20;19(4):529-40. PMID: 22520759.
Zhang J, Deng X, Choi HG, et al. Characterization of TAE684 as a potent LRRK2 kinase inhibitor. Bioorg Med Chem Lett. 2012 Mar 1;22(5):1864-9. PMID: 22335897.
Cerchietti L, Damm-Welk C, Vater I, et al. Inhibition of anaplastic lymphoma kinase (ALK) activity provides a therapeutic approach for CLTC-ALK-positive human diffuse large B cell lymphomas. PLoS One. 2011 Apr 8;6(4):e18436. PMID: 21494621.
Galkin AV, Melnick JS, Kim S, et al. Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK. Proc Natl Acad Sci U S A. 2007 Jan 2;104(1):270-5. Erratum in: Proc Natl Acad Sci U S A. 2007 Feb 6;104(6):2025. PMID: 17185414.
