Canertinib CAS NO.: 267243-28-7 Canertinib.2HCL CAS NO.:289499-45-2 (Synonyms: CI-1033; PD-183805)with High Purity 99.0%Min.
Chemical Information
Quick Details:
Product Name | Canertinib |
Molecular Formula | C24H25ClFN5O3 |
Molecular Weight | 485.94 |
Storage | 3years in -20ºC |
Targets | EGFR HER2 HER4 |
IC50 | 0.8 nM 19 nM |
IC50 | 7 nM |
Dosage | / |
Product Name: Canertinib
Other Name:N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide;N-[4-(3-chloro-4-fluoro-anilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide;CI-1033(Canertinib);PD-183805;Canertinib base;Canetinib;Canertinib (CI-1033);N-[4-(3-chloro-4-fluoroanilino)-7-(3-Morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-en
Model No.: ATC-158
CAS No.: 267243-28-7
Molecular Formula: C24H25ClFN5O3
Molecular Weight:485.944
Stability: N/A
Target:N/A
Appearance: White or Nearly White Crystalline Powder
Melting Point: N/A
Purity: 99%+
Suitable People: ALl
Product Specifications: Pharmaceutical Grade
Standard: Qualified
MOQ(Minimum Order Quantity): 10g
Payment: L/C, T/T, Western Union
Shipment: EMS, DHL, FedEx, TNT
Packing: Aluminium Foil Bag or as Required
Brand: Biocar
Origion: Hubei,China
Export Markets: Global
Product Description
Canertinib is an irreversible quinazoline-based inhibitor of HER family tyrosine kinases with IC50 values of 0.8, 19 and 7 nM for EGFR, HER2 and HER4, respectively.
Canertinib (also known as CI-1033), a 3-chloro, 4-fluoro, 4-anilinoquinazoline, is an orally available, potent and irreversible Pan-erbB tyrosine kinase inhibitor that inhibits EGFR, HER2 and HER4 in vitro with the half maximal inhibition concentration IC50 of 0.8 nM, 19 nM and 7 nM respectively [1].
Canertinib irreversibly binds into the ATP pocket within the TK domain of all erbB family members, where the acrylamide side-chain at position C6 of canertinib is brought into close proximity with cysteines of erbB members, followed by the rapid formation of a covalent bond, which permanently inactivates the catalytically active erB1, erB2 and erB4 family members and effectively inhibits erbB3-dependent signaling [2].
Canertinib (CI-1033) is an experimental drug candidate 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).
Drug Interactions: 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.
Applications/Usage
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Color:White powder
Purity:99%min
Usage: Pharmaceutical intermediates
Delivery Detail:Shipped in 3 days after payment
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