Name: Canertinib
Brand: BOC Sciences
Rating: 5 (1 reviews)

Canertinib

Category	Orthopoxvirus
CAS	267243-28-7
Description	Canertinib 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).

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Product Information

Synonyms

CI-1033; PD-183805; N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide; N-[4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide; 2-propenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-

IUPAC Name

N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide

Molecular Weight

485.94

Molecular Formula

C24H25ClFN5O3

Canonical SMILES

C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4

InChI

InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)

InChIKey

OMZCMEYTWSXEPZ-UHFFFAOYSA-N

Boiling Point

691.0±55.0°C (Predicted)

Melting Point

188-190°C

Flash Point

371.7±31.5 °C

Purity

>98%

Density

1.355±0.06 g/cm3 (Predicted)

Solubility

Soluble in DMSO, Methanol

Appearance

Pale Yellow Solid

Storage

Store at -20°C

Complexity

671

Exact Mass

485.1629955

Index Of Refraction

1.650

In Vitro

Canertinib significantly inhibits growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner.
IC50 is approximately 0.8 μM and by 5μM both cell lines are completely growth-arrested within 72 h of treatment. Incubation of exponentially growing RaH3 and RaH5 with 1 μM canertinib accumulated the cells in the G1-phase of the cell cycle within 24 h of treatment without induction of Apoptosis.
1 μM canertinib inhibits ErbB1-3 receptor phosphorylation with a concomitant decrease of Akt-, Erk1/2- and Stat3 activity in both cell lines.
Canertinib also is a potent activator of exosome secretion.

In Vivo

Canertinib shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration. 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. 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.

PSA

88.61000

Target

EGFR: 7.4 nM (IC50)
ErbB: 29 nM (IC50)

Vapor Pressure

0.0±2.2 mmHg at 25°C

XLogP3-AA

3.9

Description of First Aid Measures

Eye contact

Remove any contact lenses, locate eye-wash station, and flush eyes immediately with large amounts of water. Separate eyelids with fingers to ensure adequate flushing. Promptly call a physician.

Skin contact

Rinse skin thoroughly with large amounts of water. Remove contaminated clothing and shoes and call a physician.

Inhalation

Immediately relocate self or casualty to fresh air. If breathing is difficult, give cardiopulmonary resuscitation (CPR). Avoid mouth-to-mouth resuscitation.

Ingestion

Wash out mouth with water; Do NOT induce vomiting; call a physician.

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