| Identification | Back Directory | [Name]
Canertinib | [CAS]
267243-28-7 | [Synonyms]
PD-183805
Canetinib
Canertinib base
quinazolin-6-yl)
CI-1033(Canertinib)
Canertinib (CI-1033)
-7-(3-morpholinopropoxy)
Canertinib--CI-1033, PD-183805
N-(4-((3-Chloro-4-fluorophenyl)
N-[4-(3-chloro-4-fluoro-anilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide
N-[4-(3-chloro-4-fluoroanilino)-7-(3-Morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-en
N-(4-(3-chloro-4-fluorophenylamino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide
N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide
2-PropenaMide,N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-(4-Morpholinyl)propoxy]-6-quinazolinyl]-
Canertinib N-[4-(3-Chloro-4-fluoroanilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide
N-[4-(3-Chloro-4-fluoroanilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide Canertinib (CI-1033) | [EINECS(EC#)]
1308068-626-2 | [Molecular Formula]
C24H25ClFN5O3 | [MDL Number]
MFCD09837878 | [MOL File]
267243-28-7.mol | [Molecular Weight]
485.944 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [Uses]
Antineoplastic; irreversible pan-erbB tyrosine kinase inhibitor used to treat cancer. | [Uses]
CI-1033 is a potent inhibitor of EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, respectively. | [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]. | [in vivo]
Canertinib shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration[1]. The growth of human malignant melanoma xenografts, RaH3 and RaH5, in nude mice is significantly inhibited by i.p. injections of 40 mg/kg/day canertinib (Fig. 4). The anti-proliferative effect on melanoma xenografts is visible already within 4 days of treatment and further increased throughout the treatment period as observed through the differences in tumor volumes, reaching statistical significance within 18 days of treatment[2]. | [IC 50]
EGFR: 7.4 nM (IC50); ErbB2: 9 nM (IC50) | [storage]
Store at -20°C | [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. |
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J & K SCIENTIFIC LTD.
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https://www.jkchemical.com |
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NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
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