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Postion:Product Catalog >Biochemical Engineering>Inhibitors>protein tyrosine kinase>Rociletinib
Rociletinib
  • Rociletinib

Rociletinib NEW

Price $45 $68 $126
Package 5mg 10mg 50mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Rociletinib CAS No.: 1374640-70-6
Purity: 99.25% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameRociletinib
DescriptionRociletinib (CNX-419) is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.
Cell ResearchCells are seeded at 3,000 cells per well in growth media supplemented with 5% FBS, 2 mmol/L, L-glutamine, and 1% penicillin–streptomycin, allowed to adhere overnight, and treated with a dilution series of test compounds for 72 hours. Cell viability is determined by CellTiter-Glo, and results are represented as background-subtracted relative light units normalized to a dimethyl sulfoxide (DMSO)–treated control. Growth inhibition (GI 50) values are determined by GraphPad Prism 5.04. MK-2206 and XL-880 compounds are obtained from Selleck Chemical. CI data are generated using CalcuSyn.(Only for Reference)
Kinase AssayInhibition Kinetics Studies: Recombinant human wild-type and T790M/L858R double mutant EGFR, both Nterminal GST-tagged, are used in the assay. The Omnia continuous read assay is performed as described by the vendor.
In vitroCO-1686 demonstrates significant dose-dependent tumor growth inhibition across all models of EGFR mutations, including transgenic mice expressing EGFRL858R- and EGFRL858R/T790M.
In vivoCO-1686 selectively inhibits the growth of NSCLC (non-small cell lung cancer) cells expressing mutant EGFR, with a GI50 range of 7 to 32 nM, and induces apoptosis. NSCLC cell lines resistant to CO-1686 show signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. In cells expressing mutant EGFR, CO-1686 inhibits p-EGFR with an IC50 range of 62 to 187 nM, while also inhibiting EGFR phosphorylation in three types of cells expressing WT (wild type) EGFR, with an IC50 of >2,000 nM.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (167.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
KeywordsCNX 419 | AVL 301 | HER1 | Inhibitor | inhibit | CO 1686 | EGFR | ErbB-1 | Rociletinib | AVL301 | CNX419 | Epidermal growth factor receptor | CO1686
Inhibitors RelatedOsimertinib | Lidocaine Hydrochloride hydrate | Lapatinib | Afatinib Dimaleate | Erlotinib hydrochloride | Erlotinib | Neratinib | Chalcone | Osimertinib mesylate | Genistein | Khellin | Gefitinib
Related Compound LibrariesHighly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | 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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