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AZ12253801 

Cat. No. M30698
AZ12253801  Structure
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Biological Activity

AZ12253801 is an ATP-competitive IGF-1R tyrosine kinase inhibitor that shows ∼10-fold selectivity over the insulin receptor. AZ12253801 inhibits IGF-1R–driven proliferation in 3T3 mouse fibroblasts (transfected with human IGF-1R) with an IC50 of 17 nmol/L. The IC50 for epidermal growth factor receptor (EGFR)–driven proliferation is 440 nmol/L. Anti-tumor activity.

Chemical Information
Molecular Weight 402.45
Formula C21H22N8O
CAS Number 851432-37-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Denis Krndija, et al. Biochem J. IGF1R undergoes active and directed centripetal transport on filopodia upon receptor activation

[2] Kunal A Lodhia, et al. Int J Cancer. Suppression of homologous recombination sensitizes human tumor cells to IGF-1R inhibition

[3] M M Chitnis, et al. Oncogene. IGF-1R inhibition enhances radiosensitivity and delays double-strand break repair by both non-homologous end-joining and homologous recombination

[4] Emma E Vincent, et al. PLoS One. Targeting non-small cell lung cancer cells by dual inhibition of the insulin receptor and the insulin-like growth factor-1 receptor

[5] P H S Shaw, et al. Br J Cancer. Dual inhibition of epidermal growth factor and insulin-like 1 growth factor receptors reduce intestinal adenoma burden in the Apc(min/+) mouse

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Keywords: AZ12253801  supplier, IGF-1R, inhibitors, activators

 
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