Canertinib
- CAS NO.:267243-28-7
- Empirical Formula: C24H25ClFN5O3
- Molecular Weight: 485.94
- MDL number: MFCD09837878
- EINECS: 1308068-626-2
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-07-02 08:54:57
What is Canertinib?
The Uses of Canertinib
Canertinib is a kind of irreversible pan-erbB tyrosine kinase inhibitor used to treat cancer.
The Uses of Canertinib
CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively.
The Uses of Canertinib
Antineoplastic; irreversible pan-erbB tyrosine kinase inhibitor used to treat cancer.
What are the applications of Application
Canertinib is an irreversible pan-erbB tyrosine kinase inhibitor
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.
Properties of Canertinib
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 |
Safety information for Canertinib
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for Canertinib
New Products
Tubulysin B Tubulysin H Tubulysin I 2-(azetidin-3-ylidene)acetonitrile (hydrochloride) CYCLOBUTYLAMINE HYDROCHLORIDE tetrahydro-4-methyl-2H-pyran 4-(Benzyloxy)-3-bromophenylacetic Acid 2H-Pyran, 4-ethynyltetrahydro- 3-METHYLAZETIDIN-3-OL HYDROCHLORIDE 2-[[(3aR,4S,6R,6aS)-6-Aminotetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol ethanedioate Fuel shell 2-[2-[3(S)-3[2-(7-chloro-2-quinolinyl) ethenyl] phenyl-3- hydroxyl propyl] phenyl]-2-propanol Calcium Sodium Phosphosilicate IH 2-(1-(Mercaptomethyl) cyclopropyl) acetonitrile (1R,2S)-2-(3,4-Difluorophenyl)cyclopropanamine 5-(piperazin-1-yl) benzofuran-2- carboxamide 1-(4-amino-2- methylbenzoyl)-7- chloro-3,4-dihydro- 1H-benzo[b] azepin-5(2H)-one Latanoprostene Bunod Magnesium Trisilicate Lubiprostone Flame Retardant Zinc Borate 1H-Imidazole-4-carbonitrile 7-Methoxyquinoline-4-carbonitrile 7-Methoxyquinoline-4-carboxylic acidRelated products of tetrahydrofuran
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