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Canertinib dihydrochloride

Cat. No. M3684

Canertinib dihydrochloride Structure

Synonym: CI-1033 dihydrochloride, Canertinib 2HCl, PD-183805 dihydrochloride

Size Price Availability Quantity
10mg USD 60 In stock
25mg USD 90 In stock
50mg USD 130 In stock
100mg USD 220 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Canertinib significantly inhibited growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner as determined by cell counting. Canertinib significantly inhibited growth of RaH3 and RaH5 melanoma xenografts in nude mice. Canertinib inhibited receptor autophosphorylation and kinase activity of both mutated and FLT3 ligand stimulated wildtype FLT3, leading to inhibition of the PI3-kinase and MAP kinase pathways. CI-1033 shows excellent potency for irreversible inhibition of erbB2 autophosphorylation in MDA-MB 453 cells. CI-1033 also shows high permeability in Caco-2 cells and inhibits secretory transport of vinblastine, which indicates that CI-1033 is a likely inhibitor of the P-gp.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 558.86
Formula C24H27Cl3FN5O3
CAS Number 289499-45-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo.
Djerf Severinsson EA, et al. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8. PMID: 21982771.

Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice.
Nordigården A, et al. Br J Haematol. 2011 Oct;155(2):198-208. PMID: 21848891.

A multivariate model of ErbB network composition predicts ovarian cancer cell response to canertinib.
Prasasya RD, et al. Biotechnol Bioeng. 2012 Jan;109(1):213-24. PMID: 21830205.

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Keywords: Canertinib dihydrochloride, CI-1033 dihydrochloride, Canertinib 2HCl, PD-183805 dihydrochloride supplier, EGFR/HER2, inhibitors

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