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Submit ReviewCeritinib
Description: Highly potent ALK inhibitor; also potently inhibits IR, IGF1R, STK22D and FLT3
Alternative Names: LDK378
Chemical Name: 5-Chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine
Purity: ≥98% (HPLC)
Biological Activity for Ceritinib
Ceritinib is a highly potent anaplastic lymphoma kinase (ALK) inhibitor (IC50 = 0.2 nM). Also displays potent inhibition of insulin receptor (IR), insulin-like growth factor receptor 1 (IGF1R), serine/threonine-protein kinase STK22D and FLT3 (IC50 values are 7, 8, 23 and 60 nM, respectively). Inhibits tumor growth in Karpas299 and H2228 rat xenograft models.
Technical Data for Ceritinib
| M. Wt | 558.14 |
| Formula | C28H36ClN5O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1032900-25-6 |
| PubChem ID | 57379345 |
| InChI Key | VERWOWGGCGHDQE-UHFFFAOYSA-N |
| Smiles | CC(C)OC1=C(NC2=NC=C(Cl)C(NC3=C(C=CC=C3)[S](=O)(=O)C(C)C)=N2)C=C(C)C(=C1)C1CCNCC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Ceritinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 2.79 | 5 with gentle warming | |
| ethanol | 2.79 | 5 with gentle warming |
Preparing Stock Solutions for Ceritinib
The following data is based on the product molecular weight 558.14. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.05 mM | 35.83 mL | 179.17 mL | 358.33 mL |
| 0.25 mM | 7.17 mL | 35.83 mL | 71.67 mL |
| 0.5 mM | 3.58 mL | 17.92 mL | 35.83 mL |
| 2.5 mM | 0.72 mL | 3.58 mL | 7.17 mL |
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Product Datasheets for Ceritinib
References for Ceritinib
References are publications that support the biological activity of the product.
Marsilje et al (2013) Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diam J.Med.Chem. 56 5675 PMID: 23742252
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Keywords: Ceritinib, Ceritinib supplier, LDK378, ALK, inhibitors, inhibits, highly, potent, Anaplastic, lymphoma, kinase, insulin, receptor, InsR, insulin-like, growth, factor, IGF1R, FLT3, STK22D, Insulin, and, Receptors, 6905, Tocris Bioscience
Citations for Ceritinib
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