Canertinib

Canertinib

Antitumor drugs and immunosuppressants Canertinib /phoebe@chembj.com

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

Canertinib 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.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.

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