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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 & Documentation
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.

Chemical Information
Molecular Weight 413.40
Formula C21H18F3N5O
CAS Number 879127-07-8
Solubility (25°C) DMSO ≥ 60 mg/mL
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] 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, activators


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