A selective ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines (IC50s = 2-5 nM); suppresses tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma; also inhibits the activity of the Parkinson’s disease-linked LRRK2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2

TAE684 – 50 mg

Brand:
Cayman
CAS:
761439-42-3
Storage:
-20
UN-No:
Non-Hazardous - /

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).{29085,29086} TAE684 is an ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines with IC50 values of 2-5 nM.{29085} 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.{29085} 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.{29085,29086} 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).{29087}  

 

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Description

A selective ALK inhibitor that blocks the proliferation of ALCL-derived and ALK-dependent cell lines (IC50s = 2-5 nM); suppresses tumor growth in in vivo models of ALK-positive ALCL and neuroblastoma; also inhibits the activity of the Parkinson’s disease-linked LRRK2 (IC50s = 7.8 and 6.1 nM for wild-type and G2019S mutant LRRK2, respectively)

Formal name: 5-​chloro-​N2-​[2-​methoxy-​4-​[4-​(4-​methyl-​1-​piperazinyl)​-​1-​piperidinyl]​phenyl]​-​N4-​[2-​[(1-​methylethyl)​sulfonyl]​phenyl]​-2,​4-pyrimidinediamine

Synonyms:  NVP-TAE684

Molecular weight: 614.2

CAS: 761439-42-3

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Activin-like Kinases (ALKs)||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|ALK (Activin-like Kinase) Signaling||Research Area|Neuroscience|Neurodegenerative Disorders|Parkinson’s Disease

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