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EGFR-IN-1

Catalog No. T11157   CAS 1625677-63-5

EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR.

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EGFR-IN-1 Chemical Structure
EGFR-IN-1, CAS 1625677-63-5
Pack Size Availability Price/USD Quantity
25 mg 8-10 weeks $ 1,820.00
50 mg 8-10 weeks $ 2,380.00
100 mg 8-10 weeks $ 3,100.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 cells. This compound potently inhibits Gefitinib-resistant EGFR L858R/T790M mutations with a 100-fold selectivity over the wild-type EGFR.
In vitro EGFR-IN-1 highly selective against a panel of 100 kinases.EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively. EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively.
In vivo EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM.EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight. EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg.
Molecular Weight 514.58
Formula C28H30N6O4
CAS No. 1625677-63-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92.

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Keywords

EGFR-IN-1 1625677-63-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR EGFR IN 1 EGFRIN1 inhibitor inhibit

 

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