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[CAS NO. 289499-45-2] Canertinib dihydrochloride
| 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-10367A |
| Brand: | MCE |
| CAS: | 289499-45-2 |
Overview
| MDL | MFCD09954112 |
|---|---|
| Molecular Weight | 558.86 |
| Molecular Formula | C24H27Cl3FN5O3 |
| SMILES | C=CC(NC1=CC2=C(N=CN=C2C=C1OCCCN3CCOCC3)NC4=CC=C(C(Cl)=C4)F)=O.[H]Cl.[H]Cl |
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 dihydrochloride (CI-1033 dihydrochloride) 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 dihydrochloride 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 dihydrochloride (CI-1033 dihydrochloride) 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
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 62.5 mg/mL ( 111.83 mM ; Need ultrasonic)
H 2 O : 25 mg/mL ( 44.73 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7894 mL | 8.9468 mL | 17.8936 mL |
| 5 mM | 0.3579 mL | 1.7894 mL | 3.5787 mL |
| 10 mM | 0.1789 mL | 0.8947 mL | 1.7894 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 10 mg/mL (17.89 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.72 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: 2.08 mg/mL (3.72 mM); Suspended solution; Need ultrasonic
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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