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EGFR-IN-2

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Catalog No. T11159Cas No. 1643497-70-4

EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor.

EGFR-IN-2

EGFR-IN-2

😃Good
Catalog No. T11159Cas No. 1643497-70-4
EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor.
Pack SizePriceAvailabilityQuantity
25 mg1.444 â‚¬6-8 weeks
50 mg1.881 â‚¬6-8 weeks
100 mg2.375 â‚¬6-8 weeks
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Product Introduction

Bioactivity
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.
Chemical Properties
Molecular Weight551.66
FormulaC26H33N9O3S
Cas No.1643497-70-4
Relative Density.1.53 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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