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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 0.1-0.3μM 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 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. 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.
| Cell Experiment | |
|---|---|
| Cell lines | Luciferase-expressing Karpas-299, SU-DHL-1, and Ba/F3 cells and transformed Ba/F3 stably expressing NPM-ALK, Bcr-Abl, or TEL-kinase fusion constructs. |
| Preparation method | Seeding cells in 384-well plates (2.5×104 cells per well) and incubating with serial dilutions of TAE684 or DMSO for 2–3 days. Using Luciferase expression as a measure of cell proliferation/survival and evaluating with the Bright-Glo Luciferase Assay System.Using XLFit software to generate IC50 values . |
| Concentrations | 1 nM-10 μM |
| Incubation time | 2–3 days |
| Animal Experiment | |
|---|---|
| Animal models | Karpas-299 xenografts are established in 4- to 6-week old female Fox Chase SCIDBeige mice |
| Formulation | Resuspended in 10% 1-methyl-2-pyrrolidinone/90% polyethylene glycol 300 solution |
| Dosages | 1, 3, and 10 mg/kg |
| Administration | Once daily by oral gavage for 3 weeks |
| Molecular Weight | 614.2 |
| Formula | C30H40ClN7O3S |
| CAS Number | 761439-42-3 |
| Solubility (25°C) | DMSO ≥28 mg/mL Ethanol ≥1.8 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ALK Products |
|---|
| F-1
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
| TL13-22
TL13-22 is a negative control for TL13-12 and a potent ALK inhibitor with an IC50 of 0.54 nM. |
| TL13-110
TL13-110 is a negative control for TL13-112 and a potent ALK inhibitor with an IC50 of 0.34 nM. |
| ALK inhibitor 2
ALK inhibitor 2 is a potent pyrimidin ALK inhibitor. |
| NVL-655 TFA
NVL-655 (ALK-IN-27) TFA is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 (ALK-IN-27) TFA has an IC50 of 2.7 nM. It can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
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