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Chemical Properties of 'Ceritinib' |
|
CAT No. : |
CS-O-11185 |
CAS Registry No. : | 1032900-25-6 |
Category : | API Standards |
Molecular Weight: | 558.14 |
Molecular Formula : | C₂₈H₃₆ClN₅O₃S |
OTHER INFORMATION of 'Ceritinib' |
|
Purity : | Not less than 95% |
Therapeutic : | Anti-Cancer / Oncology |
Purity : | Not less than 95% |
Therapeutic : | Anti-Cancer / Oncology |
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 |
Applicationnotes : | Ceritinib is used for the treatment of adults with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) following failure (secondary to resistance or intolerance) of prior crizotinib therapy. |
Synonym : | 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine |
References : | "Medscape, April 29, 2014; Engelman JA (2014)" |
Smileys : | CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl |
Appearance : | White to off-white solid |
Use Classification : | Human drugs -> Zykadia -> EMA Drug Category |
Hazard Class : | Acute Tox. 4 (33.33%) |
EC Number : | 811-457-8 |
UNII : | K418KG2GET |
NCI Thesaurus Code : | C115112 |
RXCUI : | 1535457 |
MeSH Entry Terms : | 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine |
Other Synonyms : | ceritinib |
Removed Synonyms : | Ceritinib dihydrochloride |
Label Ingredient : | CERITINIB |
NDC Code : | 0078-0694-48, 0078-0694-84 |
Toxicity Summary : | There is not currently any data on carcinogenicity, effect on human fertility, or on early embryonic development. However, based on its mechanism of action, ceritinib may cause fetal harm when administered to pregnant women and should therefore be administered with effective contraception during treatment. Diarrhea, nausea, vomiting, or abdominal pain occurred in 96% of 255 patients including severe cases in 14% of patients. Drug-induced hepatotoxicity also occurred in 27% of 255 patients, presenting as alanine aminotransferase (ALT) levels greater than 5 times the upper limit of normal (ULN). Severe, life-threatening, or fatal interstitial lung disease (ILD)/pneumonitis, hyperglycaemia, and bradycardia have also been reported. |
Hepatotoxicity : | Elevations in serum aminotransferase levels are common during ceritinib therapy occurring in 20% to 50% of patients, but rising above 5 times the upper limit of the normal range in only 1% to 2%. Hepatic failure is said to have occurred in 0.2% of patients and to have resulted in several fatalities. Hepatotoxicity appears to be a class effect among ALK inhibitors, although liver injury appears to be more frequent and more severe with crizotinib than ceritinib or alectinib. Specific details of the liver injury associated with ceritinib such as latency, serum enzyme pattern, clinical features and course, have not been published. Other ALK inhibitors typically cause liver injury arising within days or weeks of starting therapy, and presenting abruptly with hepatocellular enzyme elevations and a moderate-to-severe course. Immunoallergic and autoimmune features are not common. The rate of clinically significant liver injury and hepatic failure is increased in patients with preexisting cirrhosis or hepatic impairment due to liver tumor burden. Recurrence upon reexposure has been reported. |
Protein Binding : | Ceritinib is 97% bound to human plasma proteins, independent of drug concentration. |
Exact Mass : | 557.2227389 |
InChI : | InChI=1S/C28H36ClN5O3S/c1-17(2)37-25-15-21(20-10-12-30-13-11-20)19(5)14-24(25)33-28-31-16-22(29)27(34-28)32-23-8-6-7-9-26(23)38(35,36)18(3)4/h6-9,14-18,20,30H,10-13H2,1-5H3,(H2,31,32,33,34) |
InchIKey : | VERWOWGGCGHDQE-UHFFFAOYSA-N |
Canonical SMILES : | CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl |
Isomeric SMILES : | CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl |
Product Description : | Ceritinib is a member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(piperidin-4-yl)-5-methylphenyl and 2-(isopropylsulfonyl)phenyl substituents. Used for the treatment of ALK-positive metastatic non-small cell lung cancer. It has a role as an antineoplastic agent and an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor. It is an aminopyrimidine, an aromatic ether, an organochlorine compound, a secondary amino compound, a member of piperidines and a sulfone. |
Custom Duty : | Applicable |
Port of Loading : | Canada |
Expected Dispatch : | 15-Aug-2022 |
Taxes : | Not Applicable |
Refund Policy : | 30-days money back |
Custom Duty : | Applicable |
Port of Loading : | Canada |
Expected Dispatch : | 15-Aug-2022 |
Taxes : | Not Applicable |
Refund Policy : | 30-days money back |
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