Canertinib

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Chemical Information

Product name：Canertinib	Purity：98% min
CAS NO：267243-28-7	Solubility：DMSO : 4.9 mg/mL (10.08 mM)
Molecular Formula：C₂₄H₂₅ClFN₅O₃	Package：Package according to customer requirements
Molecular Weight：485.9444	Storage：Store at -20℃

Quality control

COA

Remarks

Canertinib, also known as CI1033 and PD183805, is a potent ErbB inhibitor for the treatment of cancer. It is an irreversible tyrosine-kinase inhibitor with activity against EGFR (IC50 0.8 nM), HER-2 (IC50 19 nM) and ErbB-4 (IC50 7 nM). By 2015, Pfizer had discontinued development of the drug. Canertinib has been reported as a substrate for OATP1B3. Interaction of canertinib with OATP1B3 may alter its hepatic disposition and can lead to transporter mediated drug-drug interactions. Also, canertinib is not an inhibitor of OATP-1B1 or OATP-1B3 transporter.

HER2 Inhibitors Related Products:

Poziotinib (HM781-36B); Mubritinib; Tucatinib; Canertinib dihydrochloride; Lapatinib; Lapatinib ditosylate; Afatinib (BIBW2992); Afatinib (BIBW2992) Dimaleate; CUDC-101; TAK-285; Sapitinib

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. 2000 Apr 6;43(7):1380-97.

[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.