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EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | 1.444 € | 6-8 weeks | |
50 mg | 1.881 € | 6-8 weeks | |
100 mg | 2.375 € | 6-8 weeks |
Description | EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor. |
In vitro | EGFR-IN-2 demonstrats strong antiproliferative effect on the T790M mutant carrying H1975 cell line (IC50=0.361 μM) and the single activating mutant PC9 cell line (IC50=0.151 μM). Furthermore, EGFR-IN-2 also shows good selectivity against other kinases when evaluated in a 225-kinase panel (12/225 kinases inhibited at >70% when tested at 0.1 μM, 61-fold over the TMLR Ki and 63-fold over the TMdel Ki).In addition, EGFR-IN-2 inhibits EGFR autophosphorylation with IC50s of 0.027 μM, 0.009 μM ,0.033 μM , and 0.218 μM in double mutant TMLR cell line H1975, double mutant TMdel cell line PC9-ER, activating mutant del |
In vivo | To examine its inhibitory effect on pEGFR levels in vivo, EGFR-IN-2 is studied in a mouse H1975 (TMLR) xenograft model. A single oral dose of 21 at 50 mg/kg sustains free plasma concentrations of EGFR-IN-2 at or exceeding the in vitro p-EGFR IC50 (0.027 μM) for over 8 hours, and a 100 mg/kg dose extends coverage to the last measured time point at 16 hours post-dose. Corresponding knockdown of p-EGFR, pERK1/2, and AKT levels at these time points suggests target engagement in vivo. |
Molecular Weight | 551.66 |
Formula | C26H33N9O3S |
Cas No. | 1643497-70-4 |
Relative Density. | 1.53 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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