Ceritinib

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Cat.No. 6905 - Ceritinib | C28H36ClN5O3S | CAS No. 1032900-25-6
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)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

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

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

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

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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References

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 J.Med.Chem. 56 5675 PMID: 23742252


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View all ALK Inhibitors

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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