ChemicalBook > CAS DataBase List > Canertinib

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
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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
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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.

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N-Bromosuccinimide Price

TCI Chemical
Product number
C3818
Product name
Canertinib
Packaging
25MG
Price
$180
Updated
2025/07/31
TRC
Product number
C175600
Product name
Canertinib
Packaging
10mg
Price
$65
Updated
2021/12/16
ApexBio Technology
Product number
A1845
Product name
Canertinib(CI-1033)
Packaging
10mg
Price
$50
Updated
2021/12/16
ApexBio Technology
Product number
A1845
Product name
Canertinib(CI-1033)
Packaging
10mM(in 1mL DMSO)
Price
$50
Updated
2021/12/16
ChemScene
Product number
CS-0121
Product name
Canertinib
Purity
98.02%
Packaging
10mg
Price
$60
Updated
2021/12/16
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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].

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)

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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Canertinib Suppliers

China 147 India 2 United Kingdom 2 United States 30 Global 181
BOC Sciences
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1-631-485-4226; 16314854226
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+1 (866) 930-6790
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+1 (866) 333-9607
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View Lastest Price from Canertinib manufacturers

Sinoway Industrial co., ltd.
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
Hebei Yanxi Chemical Co., Ltd.
Product
Canertinib 267243-28-7
Price
US $0.00/kg
Min. Order
1kg
Purity
0.99
Supply Ability
20tons
Release date
2023-10-08
Zhuozhou Wenxi import and Export Co., Ltd
Product
canertinib 267243-28-7
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-06-26

267243-28-7, CanertinibRelated Search:

AG 1478 HYDROCHLORIDE DAPH AG 18 LAVENDUSTIN A METHYL 2,5-DIHYDROXYCINNAMATE H-ARG-ARG-LEU-ILE-GLU-ASP-ASN-GLU-TYR-THR-ALA-ARG-GLY-OH AG 825 TYRPHOSTIN A25 PD 173074 Bortezomib Selumetinib GDC-0068 Erlotinib hydrochloride Olaparib AG 213 CIVENTICHEM CV-409 Canertinib dihydrochloride Canertinib

  • CS-152
  • CI-1033; PD-183805; CI1033; CI 1033; PD183805; PD 183805
  • CI-1033 (Canertinib, PD-183805)
  • CI-1033(Canertinib)
  • PD-183805
  • CI-1033; PD-183805
  • Canertinib base
  • Canetinib
  • Canertinib (CI-1033)
  • 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
  • N-[4-(3-chloro-4-fluoroanilino)-7-(3-Morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-en
  • 2-PropenaMide,N-[4-[(3-chloro-4-fluorophenyl)aMino]-7-[3-(4-Morpholinyl)propoxy]-6-quinazolinyl]-
  • N-(4-(3-chloro-4-fluorophenylamino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide
  • 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)
  • Canertinib--CI-1033, PD-183805
  • -7-(3-morpholinopropoxy)
  • N-(4-((3-Chloro-4-fluorophenyl)
  • quinazolin-6-yl)
  • Canertinib USP/EP/BP
  • ErbB-1,inhibit,Inhibitor,PD 183805,PD183805,Epidermal growth factor receptor,CI 1033,HER1,Orthopoxvirus,Canertinib,EGFR,CI1033
  • Canertinib, 10 mM in DMSO
  • 267243-28-7
  • C23H23ClFN5O3
  • Inhibitors