Cobimetinib NEW
| Price | $34 | $47 | $77 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Cobimetinib | CAS No.: 934660-93-2 |
| Purity: 99.98% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Cobimetinib |
| Description | Cobimetinib (GDC-0973) is a MEK1 inhibitor (IC50=4.2 nM) with selective and oral activity. Cobimetinib exhibits antitumor activity, inhibiting tumor cell proliferation and inducing apoptosis. |
| Cell Research | Cells are plated in quadruplicate at a density of 3,000 per well in 384-well plates in normal growth medium and allowed to adhere overnight. Compounds are added in 10 concentrations based on a 3-fold dilution series. Cell viability is measured 72 h later using the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference) |
| In vitro | METHODS: A panel of BRAF-mutant, RAS-mutant, or wild-type cell lines were treated with Cobimetinib for 96 h and cell viability was measured by Cell Death Detection ELISA Plus kit. RESULTS: Cobimetinib showed potent cellular potency in multiple tumor types, particularly in BRAF or KRAS mutant cancer cell lines. In a subset of tumor cell lines, 80% of BRAF-mutant lines (both V600E and non-V600E mutations) were sensitive to Cobimetinib (EC50<1 μmol/L), 54% of lines harboring KRAS or NRAS-carrying mutations were sensitive, and the remaining 35% of lines were sensitive. [1] METHODS: NB cell lines IMR-32, SHEP, and IMR-5 were treated with Cobimetinib (1 μM) for 4 h, and target protein expression levels were measured by Western Blot. RESULTS: Cobimetinib treatment induced dephosphorylation of c-RAF and ERK and increased phosphorylation of MEK. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, Cobimetinib (1-10 mg/kg) was administered orally to mice bearing A375.X1 or NCI-H2122 xenografts once daily for 21 days. RESULTS: In the A375.X1 BRAFV600E mutant melanoma xenograft model, treatment with a dose of Cobimetinib greater than 3 mg/kg resulted in an intense TGI, and in the NCI-H2122 KRASG12C mutant NSCLC xenograft model, treatment with up to 5 mg/kg Cobimetinib resulted in a moderate TGI, and treatment with 10 mg/kg approached tumor arrest. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 44 mg/mL (82.8 mM) DMSO : 16.67 mg/mL (31.37 mM) |
| Keywords | XL 518 | Apoptosis | RG-7420 | MEK | GDC0973 | Inhibitor | inhibit | MAP2K | MAPKK | Mitogen-activated protein kinase kinase | XL-518 | GDC 0973 | RG 7420 | Cobimetinib |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Pain-Related Compound Library | Kinase Inhibitor Library | EMA Approved Drug Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Anti-Cancer Drug 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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