AV-412 NEW
| Price | $37 | $53 | $87 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: AV-412 | CAS No.: 451493-31-5 |
| Purity: 99.85% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | AV-412 |
| Description | AV-412 (MP412) is an EGFR inhibitor for EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M, and ErbB2, with IC50 values of 0.75, 0.79, 0.5, 2.3, and 19 nM, respectively. |
| In vitro | In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. |
| In vivo | In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth in A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. MP-412 suppressed EGFR and ErbB2 autophosphorylation at doses corresponding to its antitumor efficacy. Various dosing schedules showed significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting frequent dosing is preferable. Additionally, MP-412 exhibited significant antitumor effects on the ErbB2-overexpressing KPL-4 breast cancer cell line, which is resistant to gefitinib. These studies indicate MP-412's potential as a therapeutic for cancers expressing EGFR and ErbB2, especially those resistant to first-generation small-molecule inhibitors. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 25 mg/mL (29.36 mM) |
| Keywords | EGFR | Inhibitor | inhibit | MP 412 | HER1 | Epidermal growth factor receptor | AV-412 | AV412 | AV 412 | MP-412 | ErbB-1 |
| Inhibitors Related | Osimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound 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
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