EGFR-IN-2 NEW
| Price | $1520 | $1980 | $2500 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-04-30 |
Product Details
| Product Name: EGFR-IN-2 | CAS No.: 1643497-70-4 |
| Supply Ability: 10g | Release date: 2025/04/30 |
Product Introduction
Bioactivity
| Name | EGFR-IN-2 |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Keywords | EGFR-IN-2 | EGFRIN2 | EGFR IN 2 | EGFR |
| Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
Company Profile Introduction
TargetMol Chemicals Inc. is headquartered in Boston, MA, and specializes in products and services that serve the research needs of chemical and biological scientists worldwide. With a client base in 40+ countries, TargetMol has evolved into one of the biggest global research suppliers for compound libraries and small molecule compounds.
170+ Compound Libraries， 10000+ Noval Small Molecucles，16000+ Nature Compounds
TargetMol diligently updates and offers over 170 types of compound libraries and a wide range of high-quality research chemicals, including inhibitors, activators, natural products, peptides, antibodies , and novel life-science kits for laboratory and scientific use. In addition, our lab allows us to conduct CADD (computer-aided drug design) and chemical synthesis to meet the customization needs of our clients.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, Massachusetts, USA
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