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AZD4625

Cat. No. M21080
AZD4625 Structure
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Quality Control & Documentation
Biological Activity

AZD4625 is a highly potent, selective, covalent and metabotropic inhibitor of the mutant GTPase KRASG12C. AZD4625 has high oral bioavailability. It is being developed to study advanced solid malignancies.

Chemical Information
Molecular Weight 486.90
Formula C24H21ClF2N4O3
Solubility (25°C) N/A
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] Atanu Chakraborty, et al. Mol Cancer Ther. AZD4625 is a Potent and Selective Inhibitor of KRASG12C

[2] Jason G Kettle, et al. J Med Chem. Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C

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  Catalog
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