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CEP-28122

Chemical Structure : CEP-28122

CAS No.: 1022958-60-6

CEP-28122 (CEP28122)

Catalog No.: PC-45404Not For Human Use, Lab Use Only.

CEP-28122 is a highly potent and selective, orally active ALK inhibitor with IC50 of 1.9 nM.

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Biological Activity

CEP-28122 is a highly potent and selective, orally active ALK inhibitor with IC50 of 1.9 nM.
CEP-28122 exhibits no-to-weak inhibition against a panel of 259 kinases and only 15 kinases showes >90% inhibition at 1 uM.
CEP-28122 shows growth inhibition/cytotoxicity of ALCL, NSCLC, and neuroblastoma cells, and displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice (30 mg/kg).

Physicochemical Properties

M.Wt 539.0689
Formula C28H35ClN6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Bicyclo[2.2.1]hept-5-ene-2-carboxamide, 3-[[5-chloro-2-[[(7S)-6,7,8,9-tetrahydro-1-methoxy-7-(4-morpholinyl)-5H-benzocyclohepten-2-yl]amino]-4-pyrimidinyl]amino]-, (1S,2S,3R,4R)-

References

1. Cheng M, et al. Mol Cancer Ther. 2012 Mar;11(3):670-9.

2. Sullivan I, et al. Ther Adv Med Oncol. 2016 Jan;8(1):32-47.

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