Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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EGFR-IN-1 1625677-63-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR EGFR IN 1 EGFRIN1 inhibitor inhibit