Canertinib
Canertinib
CAS: 267243-28-7
Molecular Formula: C24H25ClFN5O3
Canertinib - Names and Identifiers
| Name | Canertinib |
| Synonyms | CS-152 CI1033 CI-1033 CI 1033 PD-183805 Canetinib PD183805 PD-183805 PD 183805 Canertinib Canertinib base CI-1033(Canertinib) CI-1033 (Canertinib, PD-183805) N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[2-(morpholin-4-yl)ethoxy]quinazolin-6-yl}prop-2-enamide N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide |
| CAS | 267243-28-7 |
| EINECS | 1308068-626-2 |
| InChI | InChI=1/C23H23ClFN5O3/c1-2-22(31)29-20-12-16-19(13-21(20)33-10-7-30-5-8-32-9-6-30)26-14-27-23(16)28-15-3-4-18(25)17(24)11-15/h2-4,11-14H,1,5-10H2,(H,29,31)(H,26,27,28) |
Canertinib - Physico-chemical Properties
| Molecular Formula | C24H25ClFN5O3 |
| Molar Mass | 485.94 |
| Density | 1.355±0.06 g/cm3(Predicted) |
| Melting Point | 188-190° |
| Boling Point | 691.0±55.0 °C(Predicted) |
| Flash Point | 364.2°C |
| Solubility | Soluble in DMSO (2 mg/ml), methanol, ethanol (9 mg/ml), and water (<1 mg/ml). |
| Vapor Presure | 2.86E-18mmHg at 25°C |
| Appearance | White or similar to white crystalline powder |
| pKa | 12.09±0.43(Predicted) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Refractive Index | 1.659 |
| In vitro study | CI-1033 acts on MDA-MB 453 cells and effectively inhibits erbB2 autophosphorylation, which is irreversible. CI-1033 acts on Caco-2 cells with high permeability and inhibits the secretory transport of vinblastine, indicating that CI-1033 is a class of P-gp inhibitors. CI-1033 alone acted on MDA-MB-453 cells, significantly inhibited constitutively activated Akt and MAPK, and enhanced p27 expression. The combination of CI-1033 and gemcitabine acts on MDA-MB-453 cells to inhibit Akt, block the activation of MAPK phosphorylation, and promote p38 phosphorylation. CI-1033 high specificity acts on the erbB receptor family, but has no effect on PGFR, FGFR or IR at 50 μm. CI-1033 effectively inhibited A431 cells expressing EGFR with an IC50 of 7.4 nM. CI-1033 blocking heregulin-stimulated tyrosine phosphorylation of erbB2, erbB3, and erbB4, the IC50 was 5, 14, and 10 nM, respectively. CI-1033 also inhibited pp62c-fos expression in response to heregulin. CI-1033 covalently modify Cys773 at the ATP binding site of HER2 kinase and enhance cleavage of mature and immature ErbB-2 molecules. CI-1033 significantly reduced EGFR phosphorylation at tyrosine 845 and 1068 sites. These two sites respond to Src and Ras/MAPK signals, respectively. At CI-1033 concentrations of 3 µm or higher, Her-2 is dephosphorylated at tyrosine 877 and 1248 sites. CI-1033 can inhibit EGFR internalization and increase the apoptosis rate of primary internalized cells. CI-1033 at 0.1 nM significantly inhibited the proliferation of TT, TE2, TE6 and TE10 cells. |
| In vivo study | 5 mg/kg CI-10335 has significant activity in nude mice carrying A431 transplanted tumor. CI-1033 (20 to 80 mg/kg/day) in H125 xenograft models resulted in tumor regression. Oral treatment of nude mice bearing transplanted tumors of TT,TE6 and TE10 CI-1033 significantly inhibited growth, but no animals died and weight loss was <10%. |
Canertinib - Introduction
Canertinib (CI-1033;PD-183805) is an effective and irreversible EGFR inhibitor. IC50 values for inhibiting EGFR and ErbB2 autophosphorylation in cells are 7.4 and 9 nM respectively.
Last Update：2022-10-16 17:24:09
Canertinib - Reference Information
| biological activity | Canertinib (CI-1033, PD183805) is a pan-ErbB inhibitor that acts on EGFR and ErbB2,IC50 is 1.5 nM and 9.0 nM respectively, but has no inhibitory activity on PDGFR,FGFR,InsR,PKC, and CDK1/2/4. Phase 3. |
| Target | Value |
| EGFR (Cell-free assay) | 1.5 nM |
| ErbB2 (Cell-free assay) | 9.0 nM |
Last Update：2024-04-09 19:05:11
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Spot supply
Product Name: Canertinib Visit Supplier Webpage Request for quotationCAS: 267243-28-7
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Canertinib Visit Supplier Webpage Request for quotationCAS: 267243-28-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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