Ceritinib

Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency[1][2].

Product Specifications

CAS Number

[1032900-25-6]

Product Name Alternative

LDK378

UNSPSC

12352005

Hazard Statement

H302, H315, H320, H335

Target

Anaplastic lymphoma kinase (ALK) ; IGF-1R; Insulin Receptor

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Endocrinology

Assay Protocol

https://www.medchemexpress.com/LDK378.html

Purity

99.95

Solubility

DMSO : 12.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3

Molecular Formula

C28H36ClN5O3S

Molecular Weight

558.14

Precautions

H302, H315, H320, H335

References & Citations

[1]Marsilje TH, et al. 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-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013 Jul 25;56 (14) :5675-90.|[2]Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56 (14) :5673-4.|[3]Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11 (8) :996-1006.|[4]Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3 (6) :379-81.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Launched

Citation 01

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