Ceritinib

Name: Ceritinib
Brand: Tocris Bioscience
SKU: 6905

Tocris Bioscience, part of Bio-Techne | Catalog # 6905

COA / SDS

Highly potent ALK inhibitor; also potently inhibits IR, IGF1R, STK22D and FLT3

Key Product Details

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)
Molecular Weight:	558.14

View Full Technical Details for Ceritinib

Technical Data
Citations

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 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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References for Ceritinib

References are publications that support the biological activity of the product.

Marsilje 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. 2013 PMID: 23742252