DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 558.86
Formula: C24 H27 Cl3 F N5 O3
CAS Number: 289499-45-2
InChi Key: JZZFDCXSFTVOJY-UHFFFAOYSA-N
InChi: InChI=1S/C24H25ClFN5O3.2ClH/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);2*1H
Smiles: Cl.Cl.C=CC(=O)NC1=CC2=C(NC3=CC(Cl)=C(F)C=C3)N=CN=C2C=C1OCCCN1CCOCC1
Purity: 98.0
Solubility: 10 mM in DMSO
Appearance: Solid Power
Shelf Life: 1.0 years
Description:
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.