TAE684

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP01828CAS No. ：761439-42-3Purity：98%

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CAS No.	761439-42-3	Cat. No.	BCP01828
Name	TAE684
Synonyms	NVP-TAE684;TAE 684;TAE-684;
SMILES
Chemical Name
Formula	C30H40ClN7O3S	M. Wt	614.2
Purity	98%	Storage	Store at 4-8°C
Description	TAE684 does not exhibit significant cross-reactivity against other kinases. TAE684 potently inhibits the proliferation of Ba/F3 NPM-ALK cells with IC50 of 3 nM, without affecting the survival of Ba/F3 cells even at 1 μM. TAE684 also inhibits proliferation of NPM-ALK-expressing human ALCL cell lines including Karpas-299 and SU-DHL-1 with IC50 of 2–5 nM. Molecular modeling reveals that L258 may be one of the major kinase-selectivity determinants for TAE684. TAE684 treatment results in a rapid and sustained inhibition of phosphorylation of NPM-ALK. TAE684 induces apoptosis and G1 phase arrest in NPM-ALK-expressing Ba/F3 cells and ALCL patient cell lines.TAE684 markedly overcomes Crizotinib-resistance in H3122 CR cells, harboring the fusion oncogene EML4-ALK, decreasing cell growth, suppressing ALK phosphorylation and inducing apoptosis.Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM.