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EGFR inhibitor 324674

Cat. No. M9642
EGFR inhibitor 324674 Structure
Synonym:

EGFR-IN-12

Size Price Availability Quantity
5mg USD 180  USD180 In stock
10mg USD 300  USD300 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

EGFR inhibitor 324674 (EGFR-IN-12) is a cell permeable, potent and selective EGFR inhibitor with IC50 of 21 nM. EGFR inhibitor 324674 (EGFR-IN-12) inhibits mutant EGFRL858R and EGFRL861Q with IC50s of 63 nM and 4 nM, respectively. EGFR inhibitor 324674 (EGFR-IN-12) also inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 µM and 1.04 µM, respectively.

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 413.40
Formula C21H18F3N5O
CAS Number 879127-07-8
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Zhiwei Yu, et al. Biochem Biophys Res Commun. Novel irreversible EGFR tyrosine kinase inhibitor 324674 sensitizes human colon carcinoma HT29 and SW480 cells to apoptosis by blocking the EGFR pathway

[2] Qiong Zhang, et al. J Am Chem Soc. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library

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Keywords: EGFR inhibitor 324674, EGFR-IN-12 supplier, EGFR/HER2, inhibitors

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