Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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L127618-5mg | 5mg | In stock | $53.90 | |
L127618-25mg | 25mg | In stock | $108.90 | |
L127618-100mg | 100mg | In stock | $162.90 | |
L127618-250mg | 250mg | In stock | $366.90 | |
L127618-1g | 1g | In stock | $815.90 |
Highly potent ALK inhibitor; also potently inhibits IR, IGF1R, STK22D and FLT3
Synonyms | K418KG2GET | 5-chloro-2-N-[5-methyl-4-(piperidin-4-yl)-2-(propan-2-yloxy)phenyl]-4-N-[2-(propane-2-sulfonyl)phenyl]pyrimidine-2,4-diamine | 5-chloro-N(2)-{5-methyl-4-(piperidin-4-yl)-2-[(propan-2-yl)oxy]phenyl}-N(4)-[2-(propane-2-sulfonyl)phenyl]pyrimidin |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | 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 (IC50values are 7, 8, 23 and |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor) |
Note | 5mg卖完停产,不再备货 |
Product Description | LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. application: 5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine, is a Anaplastic lymphoma kinase (ALK) inhibitor. |
ALogP | 6.4 |
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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 |
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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) |
InChi Key | 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 |
PubChem CID | 57379345 |
Molecular Weight | 558.14 |
PubChem CID | 57379345 |
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ChEMBL Ligand | CHEMBL2403108 |
Wikipedia | Ceritinib |
CAS Registry No. | 1032900-25-6 |
RCSB PDB Ligand | 4MK |
PEP | ceritinib |
DrugCentral Ligand | 4866 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
I2219077 | Certificate of Analysis | Jul 12, 2024 | L127618 |
I2219078 | Certificate of Analysis | Jul 12, 2024 | L127618 |
I2219079 | Certificate of Analysis | Jul 12, 2024 | L127618 |
I2219080 | Certificate of Analysis | Jul 12, 2024 | L127618 |
I2219081 | Certificate of Analysis | Jul 12, 2024 | L127618 |
K2123541 | Certificate of Analysis | Sep 19, 2023 | L127618 |
K2124048 | Certificate of Analysis | Sep 19, 2023 | L127618 |
J1526065 | Certificate of Analysis | May 10, 2023 | L127618 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 2.79, Max Conc. mM: 5 with gentle warming; Solvent:ethanol, Max Conc. mg/mL: 2.79, Max Conc. mM: 5 with gentle warming |
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Pictogram(s) | GHS08, GHS09, GHS07 |
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Signal | Danger |
Hazard Statements | H302:Harmful if swallowed H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child |
Precautionary Statements | P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
1. Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M et al.. (2013) 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, 56 (14): (5675-90). [PMID:23742252] |
2. Shaw AT, Kim DW, Mehra R, Tan DS, Felip E, Chow LQ, Camidge DR, Vansteenkiste J, Sharma S, De Pas T et al.. (2014) Ceritinib in ALK-rearranged non-small-cell lung cancer.. N Engl J Med, 370 (13): (1189-97). [PMID:24670165] |
3. Thomas RK. (2014) Overcoming drug resistance in ALK-rearranged lung cancer.. N Engl J Med, 370 (13): (1250-1). [PMID:24670172] |
4. Friboulet L, Li N, Katayama R, Lee CC, Gainor JF, Crystal AS, Michellys PY, Awad MM, Yanagitani N, Kim S et al.. (2014) The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer.. Cancer Discov, 4 (6): (662-673). [PMID:24675041] |