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EGFR T790M/L858R-IN-2

Cat. No. M42077
EGFR T790M/L858R-IN-2 Structure
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Quality Control & Documentation
Biological Activity

EGFRT790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively.

Chemical Information
Molecular Weight 497.57
Formula C28H28FN7O
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] Jingyi He et al. Int J Oncol. Mechanisms and management of 3rd‑generation EGFR‑TKI resistance in advanced non‑small cell lung cancer (Review)

[2] Alessandro Leonetti et al. Br J Cancer. Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer

[3] J Remon et al. Ann Oncol. Osimertinib and other third-generation EGFR TKI in EGFR-mutant NSCLC patients

[4] Shang-Gin Wu et al. Mol Cancer. Management of acquired resistance to EGFR TKI-targeted therapy in advanced non-small cell lung cancer

[5] Darren A E Cross et al. Cancer Discov. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer

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Keywords: EGFR T790M/L858R-IN-2 supplier, EGFR/HER2, inhibitors, activators


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