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EAI001 

Cat. No. M30826
EAI001  Structure
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Quality Control & Documentation
Biological Activity

EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer.

Chemical Information
Molecular Weight 349.41
Formula C19H15N3O2S
CAS Number 892772-75-7
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light, dry, sealed
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] Aziz Unnisa, et al. Anticancer Agents Med Chem. Recent Advances in Epidermal Growth Factor Receptor Inhibitors (EGFRIs) and their Role in the Treatment of Cancer: A Review

[2] Swastika Maity, et al. Pharmacol Rep. Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance

[3] Shanhe Wan, et al. J Biomol Struct Dyn. Insight into binding mechanisms of EGFR allosteric inhibitors using molecular dynamics simulations and free energy calculations

[4] Peng Zhao, et al. Biochem Biophys Res Commun. Crystal structure of EGFR T790M/C797S/V948R in complex with EAI045

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  Catalog
Abmole Inhibitor Catalog




Keywords: EAI001  supplier, EGFR/HER2, inhibitors, activators


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