Canertinib
- Product Name
- Canertinib
- CAS No.
- 267243-28-7
- Chemical Name
- Canertinib
- Synonyms
- CS-152;PD-183805;Canetinib;Canertinib base;quinazolin-6-yl);CI-1033; PD-183805;CI-1033(Canertinib);Canertinib (CI-1033);Canertinib USP/EP/BP;-7-(3-morpholinopropoxy)
- CBNumber
- CB01458390
- Molecular Formula
- C24H25ClFN5O3
- Formula Weight
- 485.94
- MOL File
- 267243-28-7.mol
Canertinib Property
- Melting point:
- 188-190°
- Boiling point:
- 691.0±55.0 °C(Predicted)
- Density
- 1.355±0.06 g/cm3(Predicted)
- storage temp.
- Inert atmosphere,Store in freezer, under -20°C
- solubility
- insoluble in H2O; ≥10.1 mg/mL in EtOH; ≥12.15 mg/mL in DMSO with gentle warming
- form
- Yellow powder.
- pka
- 12.09±0.43(Predicted)
- color
- Light yellow to yellow
- CAS DataBase Reference
- 267243-28-7
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- C175600
- Product name
- Canertinib
- Packaging
- 10mg
- Price
- $65
- Updated
- 2021/12/16
- Product number
- A1845
- Product name
- Canertinib(CI-1033)
- Packaging
- 10mg
- Price
- $50
- Updated
- 2021/12/16
- Product number
- A1845
- Product name
- Canertinib(CI-1033)
- Packaging
- 10mM(in 1mL DMSO)
- Price
- $50
- Updated
- 2021/12/16
- Product number
- CS-0121
- Product name
- Canertinib
- Purity
- 98.02%
- Packaging
- 10mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- A1845
- Product name
- Canertinib(CI-1033)
- Packaging
- 50mg
- Price
- $85
- Updated
- 2021/12/16
Canertinib Chemical Properties,Usage,Production
Uses
CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
Uses
Antineoplastic; irreversible pan-erbB tyrosine kinase inhibitor used to treat cancer.
Uses
Canertinib is a kind of irreversible pan-erbB tyrosine kinase inhibitor used to treat cancer.
Definition
ChEBI: A quinazoline compound having a 3-chloro-4-fluoroanilino group at the 4-position, a propenamido group at the 6-position, and a 3-morpholinopropoxy group at the 7-position.
Biological Activity
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].
References
[1] michelle arkin, mark m. moasser. her2 directed small molecule antagonists. curr opin investig drugs. author manuscript; available in pmc 2011 february 1. published in final edited form as: curr opin investig drugs. 2008 december; 9(12): 1264–1276.
[2] calvo e, tolcher aw, hammond la, patnaik a, de bono js, eiseman ia, olson sc, lenehan pf, mccreery h, lorusso p, rowinsky ek. administration of ci-1033, an irreversible pan-erbb tyrosine kinase inhibitor, is feasible on a 7-day on, 7-day off schedule: a phase i pharmacokinetic and food effect study. clin cancer res. 2004 nov 1;10(21):7112-20.
Canertinib Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from Canertinib manufacturers
- Product
- Canertinib 267243-28-7
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 20tons
- Release date
- 2024-12-20
- Product
- Canertinib 267243-28-7
- Price
- US $0.00/kg
- Min. Order
- 1kg
- Purity
- 0.99
- Supply Ability
- 20tons
- Release date
- 2023-10-08
- Product
- CANERTINIB
- Price
- US $1.10/g
- Min. Order
- 1g
- Purity
- 99.9%
- Supply Ability
- 100 Tons Min
- Release date
- 2021-07-06