NVP-TAE684

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Hersteller AbMole
Kategorie
Typ Inhibitors
Specific against other
Menge 50mg
ArtNr M3781-50mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Cas #
761439-42-3
Bioactivity information
TAE684 is a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant). TAE684 substantially inhibits Ser910 and Ser935 phosphorylation of both wild-type LRRK2 and G2019S mutant at a concentration of 0.1-0.3uM in cells and in mouse spleen and kidney, but not in brain, following oral doses of 10mg/kg. 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 uM. 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. be one of the major kinase-selectivity determinants for TAE684. Neurite outgrowth induced by expression of the mALK R1279Q mutant could be completely inhibited by TAE684 at 30 nM.
Target
ALK
MW
614, 2
Formula
C30H40ClN7O3S
Solubility
DMSO >=28 mg/mL, Ethanol >=1.8 mg/mL
Purity
>98%

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Menge: 50mg
Lieferbar: Out of stock
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