EGFR-IN-2 NEW
| Price | $1520 | $2280 |
| Package | 25mg | 50mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2025-07-26 |
Product Details
| Product Name: EGFR-IN-2 | CAS No.: 1643497-70-4 |
| Purity: 98.52% | Supply Ability: 10g |
| Release date: 2025/07/26 |
Product Introduction
Bioactivity
| Name | EGFR-IN-2 |
| Description | EGFR-IN-2 is a non-covalent, orally available and mutation-selective EGFR inhibitor for the treatment of non-small cell lung cancer (NSCLC), with high selectivity for resistant single and double mutant T790M with IC50 = 27 nm to 33 nM, and low inhibitory activity for wild-type H292 (IC50 = 218 nM). |
| In vitro | EGFR-IN-2 (Compound 21) demonstrated excellent inhibitory activity in various EGFR-mutant NSCLC cell lines. Inhibition of EGFR autophosphorylation was evaluated in H1975 (T790M/L858R), PC9-ER (T790M/del746–750), and PC9 (del746–750) cell lines, with IC?? values of 0.027 μM, 0.008 μM, and 0.033 μM respectively. In a kinase panel of 225 kinases, only 12 were inhibited >70% at 0.1 μM, demonstrating high target specificity. EGFR-IN-2 exhibited low clearance in human liver microsomes and hepatocytes (3.8 and 2.7 mL/min/kg, respectively), and good predicted oral bioavailability [1]. |
| In vivo | In a H1975 xenograft mouse model, EGFR-IN-2 was evaluated for in vivo target engagement and pharmacokinetics. After oral administration at 50 mg/kg, free plasma concentrations remained above the in vitro IC?? (0.027 μM) for up to 8 hours; at 100 mg/kg, this duration extended to 16 hours. Corresponding suppression of phosphorylated EGFR, ERK1/2, and AKT confirmed effective target inhibition in vivo. The EGFR-IN-2 exhibited moderate plasma clearance in mice (104 mL/min/kg) with 19% oral bioavailability, and in dogs, clearance was 13 mL/min/kg with 30% bioavailability[1]. |
| Storage | store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Keywords | EGFRIN2 | EGFR IN 2 | EGFR |
| Inhibitors Related | (S)-Afatinib | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Afatinib | Chalcone | Genistein | Gefitinib |
| Related Compound Libraries | Kinase Inhibitor Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, USA
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