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Axon 2294
CAS [1472795-20-2]
MF C30H37ClN8O4MW 609.12
Potent and selective dual ALK (anaplastic lymphoma kinase ) and ACK1 inhibitor (IC50 values 12 nM and 4 nM for ALK and Ack1, respectively) with good drug-like properties: good water-solubility with moderate plasma protein binding and low brain exposure. It has good liver microsomal stability and little to no CYP inhibition. KRCA0008 also shows promising pharmacokinetic parameters in both mice and rat (oral bioavailability = 66-94.5%) and a modest tumor growth inhibition in vivo activity in H3122 human lung cancer bearing mice model comparable to Crizotinib (Axon 1660) without significant body weight change.
1,1'-(4,4'-(4,4'-(5-chloropyrimidine-2,4-diyl)bis(azanediyl)bis(3-methoxy-4,1-phenylene))bis(piperazine-4,1-diyl))diethanone
[1472795-20-2]
The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.
Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!
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