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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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C125447-10mg | 10mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $58.90 | |
C125447-50mg | 50mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $94.90 | |
C125447-250mg | 250mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $427.90 |
Synonyms | PD-183805 | EC-000.2258 | BDBM4779 | N-(4-(3-chloro-4-fluorophenylamino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide | AC-28654 | Canertinib [INN] | NCGC00182713-18 | GTPL5675 | Canertinib - CI-1033 | HMS3244N17 | N-[4-(3-chloro-4-fluoro-anilino)-7- |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Canertinib is a potent and selective inhibitor of tyrosine residue phosphorylation of EGFR, blocking signal transgression and ceasing angiogenisis. Canertinib displays an IC50 = 1.5nM. Additionally, Canertinib’s action in inhibiting EGFR increases apoptos |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of epidermal growth factor receptor;Inhibitor of erb-b2 receptor tyrosine kinase 2 |
Note | 卖完停产,不再备货 |
Product Description | Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide |
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INCHI | InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29) |
InChi Key | OMZCMEYTWSXEPZ-UHFFFAOYSA-N |
Canonical SMILES | C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 |
Isomeric SMILES | C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4 |
PubChem CID | 156414 |
Molecular Weight | 485.94 |
CAS Registry No. | 267243-28-7 |
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Wikipedia | Canertinib |
DiscoveRx TREEspot | CI-1033| |
PubChem CID | 156414 |
ChEMBL Ligand | CHEMBL31965 |
Reactome Reaction | R-HSA-1220611, R-HSA-1225978, R-HSA-9652264, R-HSA-9665121 |
Reactome Drug | R-ALL-1227677 |
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Solubility | Soluble in DMSO (2 mg/ml), methanol, ethanol (9 mg/ml), and water (<1 mg/ml). |
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1. Smaill JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW, Elliott WL et al.. (2000) Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.. J Med Chem, 43 (7): (1380-97). [PMID:10753475] [10.1021/op500134e] |
2. Rao GS, Murray S, Ethier SP. (2000) Radiosensitization of human breast cancer cells by a novel ErbB family receptor tyrosine kinase inhibitor.. Int J Radiat Oncol Biol Phys, 48 (5): (1519-28). [PMID:11121658] [10.1021/op500134e] |
3. Allen LF, Lenehan PF, Eiseman IA, Elliott WL, Fry DW. (2002) Potential benefits of the irreversible pan-erbB inhibitor, CI-1033, in the treatment of breast cancer.. Semin Oncol, 29 (3 Suppl 11): (11-21). [PMID:12138393] [10.1021/op500134e] |
4. Rixe O, Franco SX, Yardley DA, Johnston SR, Martin M, Arun BK, Letrent SP, Rugo HS. (2009) A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer.. Cancer Chemother Pharmacol, 64 (6): (1139-48). [PMID:19294387] [10.1021/op500134e] |
5. Trinks C, Severinsson EA, Holmlund B, Gréen A, Gréen H, Jönsson JI, Hallbeck AL, Walz TM. (2011) The pan-ErbB tyrosine kinase inhibitor canertinib induces caspase-mediated cell death in human T-cell leukemia (Jurkat) cells.. Biochem Biophys Res Commun, 410 (3): (422-7). [PMID:21669187] [10.1021/op500134e] |
6. Nordigården A, Zetterblad J, Trinks C, Gréen H, Eliasson P, Druid P, Lotfi K, Rönnstrand L, Walz TM, Jönsson JI. (2011) Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice.. Br J Haematol, 155 (2): (198-208). [PMID:21848891] [10.1021/op500134e] |