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LDK-378 is an anaplastic lymphoma kinase (ALK) inhibitor that displays anticancer chemotherapeutic activity. LDK-378 is used to treat ALK-positive non-small cell lung cancer (NSCLC), particularly in subjects experiencing resistance to crizotanib. This compound also inhibits IGF-1R.
| Cas No. | 1032900-25-6 |
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| Purity | ≥99% |
| Formula | C28H36ClN5O3S |
| Formula Wt. | 558.13 |
| IUPAC Name | 5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine |
| Synonym | LDK-378, Ceritinib |
| Solubility | DMSO 20 mg/mL warmed (35.83 mM) Ethanol 3 mg/mL (5.37 mM) Water Insoluble |
| Appearance | off-white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
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| Info Sheet |
Iams WT, Lovly CM. Anaplastic Lymphoma Kinase as a Therapeutic Target in Non-Small Cell Lung Cancer. Cancer J. 2015 Sep-Oct;21(5):378-82. PMID: 26389762.
Nishio M, Murakami H, Horiike A, et al. Phase I Study of Ceritinib (LDK378) in Japanese Patients with Advanced, Anaplastic Lymphoma Kinase-Rearranged Non-Small-Cell Lung Cancer or Other Tumors. J Thorac Oncol. 2015 Jul;10(7):1058-66. PMID: 26010125.
Marsilje TH, Pei W, Chen B, 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. PMID: 23742252.