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Ceritinib

Chemical Structure : Ceritinib

CAS No.: 1032900-25-6

Ceritinib (LDK378, LDK-378)

Catalog No.: PC-21774Not For Human Use, Lab Use Only.

Ceritinib (LDK378) is a potent, selective and orally active anaplastic lymphoma kinase (ALK) inhibitor with enzymatic IC50 of 200 pM, overcomes crizotinib resistance in NSCLC.

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Biological Activity

Ceritinib (LDK378) is a potent, selective and orally active anaplastic lymphoma kinase (ALK) inhibitor with enzymatic IC50 of 200 pM, overcomes crizotinib resistance in NSCLC.
Ceritinib (LDK378) shows high selectivity against an enzyme panel of 30 kinases, with 80-, 70-, and 230-fold for IGF-1R, InsR, and STK22D.
Ceritinib (LDK378) effectively inhibits ALK harboring L1196M, G1269A, I1171T, and S1206Y mutations, does not overcome two crizotinib-resistant ALK mutations, G1202R and F1174C.
Ceritinib (LDK378) overcomes crizotinib resistance in non-small cell lung cancer.

Physicochemical Properties

M.Wt 558.14
Formula C28H36ClN5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine

References

1. Marsilje TH, et al. J Med Chem. 2013 Jul 25;56(14):5675-90.

2. Friboulet L, et al. Cancer Discov. 2014 Jun;4(6):662-673.

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