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Cobimetinib [934660-93-2]

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Référence NB-64-23920-50mg

Conditionnement : 50mg

Marque : Neo Biotech

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Cobimetinib

(Synonyms: XL518, RG7420, GDC-0973) Copy Product Info

Synonyms: XL518, RG7420, GDC-0973

Catalog No. T3623 Copy Product Info

Purity: 99.96%

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

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.96%

Color:White

Product Introduction

Bioactivity

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)

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	1.8821 mL	9.4107 mL	18.8214 mL	94.1070 mL
5 mM	0.3764 mL	1.8821 mL	3.7643 mL	18.8214 mL
10 mM	0.1882 mL	0.9411 mL	1.8821 mL	9.4107 mL
20 mM	0.0941 mL	0.4705 mL	0.9411 mL	4.7054 mL
50 mM	0.0376 mL	0.1882 mL	0.3764 mL	1.8821 mL

DMSO

	1mg	5mg	10mg	50mg
100 mM	0.0188 mL	0.0941 mL	0.1882 mL	0.9411 mL

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.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

XL-518XL 518RG-7420RG 7420Mitogen-activated protein kinase kinaseMEK1MEKMAPKKMAP2KInhibitorinhibitGDC0973GDC 0973CobimetinibApoptosis

Related Tags: Cobimetinib chemical structure | Cobimetinib in vivo | Cobimetinib in vitro | Cobimetinib formula | Cobimetinib molecular weight