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CEP-28122 mesylate salt (1022958-60-6 free base)

CEP-28122 mesylate salt (1022958-60-6 free base)
CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).
Catalog No. T10759
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Purity:99.79%
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CEP-28122 mesylate salt (1022958-60-6 free base)

Catalog No. T10759Alias CEP-28122 mesylate salt

CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).
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Pack SizePriceAvailabilityQuantity
1 mg$39In Stock
5 mg$79In Stock
10 mg$123In Stock
25 mg$221In Stock
50 mg$292In Stock
1 mL x 10 mM (in DMSO)$130In Stock
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Product Introduction

Bioactivity
Description
CEP-28122 mesylate salt (1022958-60-6 free base) is a highly selective orally active ALK inhibitor (IC50: 1.9 nM in an enzyme-based TRF assay).
Targets&IC50
ALK:1.9 nM
In vitro
CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 (IC50: 46 nM). CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), neuroblastoma cells, and non-small cell lung cancer (NSCLC).
In vivo
CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near-complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher.
AliasCEP-28122 mesylate salt
Chemical Properties
Molecular Weight635.17
FormulaC29H39ClN6O6S
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 6.4 mg/mL (10.08 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5744 mL7.8719 mL15.7438 mL78.7191 mL
5 mM0.3149 mL1.5744 mL3.1488 mL15.7438 mL
10 mM0.1574 mL0.7872 mL1.5744 mL7.8719 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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