6-Demethoxytangeretin is a citrus flavonoid isolated fromCitrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast ce...
ALK inhibitor 1
ALK inhibitor 1 (compound 17) is a potent pyrimidinALKinhibitor. ALK inhibitor 1 is a potent inhibitor oftestis-specific serine/threonine kinase 2(TSSK2;IC50=31nM) and focal adhesion kinase(FAK;IC50=2nM).
ALK inhibitor 2
ALK inhibitor 2 (compound 18) is a potent pyrimidinALKinhibitor. ALK inhibitor 2 is a potent inhibitor oftestis-specific serine/threonine kinase 2(TSSK2;IC50=37nM) and focal adhesion kinase(FAK;IC50=5nM).
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.
Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively.
A 83-01 is a potent inhibitor of TGF-β type I receptorALK5 kinase, type I nodal receptorALK4 and type I nodal receptorALK7, with IC50s of 12nM, 45nM and 7.5nM against the transcription induced byALK5,ALK4 and ...
Ceritinib (LDK378) is potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3.
GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.
Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
Alectinib (CH5424802) is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.
AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency.
Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and ...
CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3nM (FAK) and 120nM(ALK cellular IC50 in 75% human plasma).
Preparation of fused bicyclic 2,4-diaminopyrimidine derivatives as a du...
Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell...
PF-06463922 is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. Phase 1.
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