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JBJ-09-063

Cat. No. M21081
JBJ-09-063 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

JBJ-09-063 is an oral allogenic epidermal growth factor inhibitor currently in preclinical development for the study of non-small cell lung cancer (NSCLC) with epidermal growth factor L858R mutations. The IC50s for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S were 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM, respectively. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and drug-resistant models.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 556.65
Formula C31H29FN4O3S
CAS Number
Purity >99%
Solubility N/A
Storage at -20°C
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  Catalog
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Keywords: JBJ-09-063 supplier, EGFR/HER2, inhibitors

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