NVP-TAE684 - TAE 684 Basic information

Description

Product Name: NVP-TAE684 - TAE 684

Synonyms: NVP-TAE684 - TAE 684;5-Chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-2,4-pyrimidinediamine;NVP-TAE 684;2,4-Pyrimidinediamine, 5-chloro-N2-[2-methoxy-4-[4-(4-methyl-1-piperazinyl)-1-piperidinyl]phenyl]-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-;TAE684 (NVP-TAE684);TAE684;NV--TAE684;5-chloro-N~2~-{2-Methoxy-4-[4-(4-Methylpiperazin-1-yl)piperidin-1-yl]phenyl}-N~4~-[2-(propan-2-ylsulfonyl)phenyl]pyriMidine-2,4-diaMine

CAS: 761439-42-3

MF: C30H40ClN7O3S

MW: 614.211

EINECS: -0

Product Categories: API;Inhibitors

Mol File: 761439-42-3.mol

NVP-TAE684 - TAE 684 Structure

NVP-TAE684 - TAE 684 Chemical Properties

density 1.296

 

NVP-TAE684 - TAE 684 Usage And Synthesis

Description TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR.

Uses TAE 684 is a potent, selective, and efficacious inhibitor of NPM-ALK, a fusion protein that is a key regulator of oncogenic events that drives the survival and proliferation of anaplastic large-cell l ymphomas.

Uses Human anaplastic lymphoma kinase (ALK) is an oncogene that is amplified in neuroblastomas and when juxtaposed with various fusion partners, its constitutive kinase activity is associated with the development of a type of anaplastic large cell lymphoma (ALCL). TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM. When tested against a panel of 35 cells transformed by various tyrosine kinases, TAE684 demonstrated 100- to 1,000-fold selectivity for inhibiting ALK-driven cell proliferation. TAE684 treatment induces cell cycle arrest and apoptosis in ALK-dependent cell lines and has been used to suppress tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma. TAE684 is also reported to inhibit the activity of the Parkinson’s disease-linked leucine-rich repeat kinase 2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively).[Cayman Chemical]