Cobimetinib [934660-93-2]
Cat# T3623-1ml
Size : 1mLx10mM(inDMSO)
Brand : TargetMol
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Cobimetinib
(Synonyms: XL518, RG7420, GDC-0973) Copy Product Info
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.
Cas No. 934660-93-2
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Purity:99.96%
Color:White
COA HNMR LCMS
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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. |
| Targets & IC50 | MEK:0.9 nM |
| 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] |
| Synonyms | XL518, RG7420, GDC-0973 |
| 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) |
| Molecular Weight | 531.31 |
| Formula | C21H21F3IN3O2 |
| Cas No. | 934660-93-2 |
| Smiles | C(=O)(C1=C(NC2=C(F)C=C(I)C=C2)C(F)=C(F)C=C1)N3C[C@](O)(C3)[C@@H]4CCCCN4 |
| Relative Density. | 1.706 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 44 mg/mL (82.81 mM), Sonication is recommended. DMSO: 84.17 mg/mL (158.42 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.76 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||