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[CAS NO. 267243-28-7] Canertinib
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-10367 |
| Brand: | MCE |
| CAS: | 267243-28-7 |
Overview
| MDL | MFCD09837878 |
|---|---|
| Molecular Weight | 485.94 |
| Molecular Formula | C24H25ClFN5O3 |
| SMILES | O=C(NC1=C(C=C2C(C(NC3=CC=C(C(Cl)=C3)F)=NC=N2)=C1)OCCCN4CCOCC4)C=C |
8 Publications Citing Use of MCE
- [1]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
- [2]J Med Chem. 2019 May 9;62(9):4772-4778.
- [3]J Cell Sci. 2015 Sep 1;128(17):3317-29.
- [4]J Biol Chem. 2012 Mar 23;287(13):9742-52.
- [5]Biochemistry. 2018 Feb 27;57(8):1369-1379.
- [6]Biochemistry. 2017 Jun 13;56(23):2921-2927.
- [7]Oncotarget. 2020 Nov 3;11(44):3921-3932.
- [8]Harvard Medical School LINCS LIBRARY
Summary
IC50 & Target
|
EGFR 7.4 nM (IC 50 ) |
ErbB2 9 nM (IC 50 ) |
In Vitro
Canertinib significantly inhibits growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner. IC
50
is approximately 0.8 μM and by 5μM both cell lines are completely growth-arrested within 72 h of treatment. Incubation of exponentially growing RaH3 and RaH5 with 1 μM canertinib accumulated the cells in the G1-phase of the cell cycle within 24 h of treatment without induction of apoptosis. 1 μM canertinib inhibits ErbB1-3 receptor phosphorylation with a concomitant decrease of Akt-, Erk1/2- and Stat3 activity in both cell lines
[2]
.
Canertinib also is a potent activator of exosome secretion
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Canertinib shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration [1] . The growth of human malignant melanoma xenografts, RaH3 and RaH5, in nude mice is significantly inhibited by i.p. injections of 40 mg/kg/day canertinib (Fig. 4). The anti-proliferative effect on melanoma xenografts is visible already within 4 days of treatment and further increased throughout the treatment period as observed through the differences in tumor volumes, reaching statistical significance within 18 days of treatment [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00174356 | Pfizer |
Carcinoma, Non-Small Cell Lung
|
December 2002 | Phase 1 |
| NCT00051051 | Pfizer |
Breast Neoplasms
|
December 2002 | Phase 2 |
| NCT00050830 | Pfizer |
Lung Neoplasms
|
January 2003 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : 12.5 mg/mL ( 25.72 mM ; Need ultrasonic)
DMSO : 4.9 mg/mL ( 10.08 mM ; Need warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0579 mL | 10.2893 mL | 20.5787 mL |
| 5 mM | 0.4116 mL | 2.0579 mL | 4.1157 mL |
| 10 mM | 0.2058 mL | 1.0289 mL | 2.0579 mL |
References
- [1] Smaill JB, et al. 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.
- [2] Djerf Severinsson EA, et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8.
- [3] McAndrews KM, et, al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52.
- [4] Smee DF, et, al. Progress in the discovery of compounds inhibiting orthopoxviruses in animal models. Antivir Chem Chemother. 2008;19(3):115-24.
Synonyms
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