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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
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
10mg USD 50  USD50 In stock
50mg USD 80  USD80 In stock
100mg USD 110  USD110 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 558.86
Formula C24H27Cl3FN5O3
CAS Number 289499-45-2
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Djerf Severinsson EA, et al. Biochem Biophys Res Commun. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo.

[2] Nordigården A, et al. Br J Haematol. Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice.

[3] Prasasya RD, et al. Biotechnol Bioeng. A multivariate model of ErbB network composition predicts ovarian cancer cell response to canertinib.

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


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