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Cobimetinib

Name: Cobimetinib
Brand: TargetMol
SKU: T3623
Price: 477 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3623Cas No. 934660-93-2

Alias XL518, RG7420, GDC-0973

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.

Cobimetinib

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Purity: 99.61%

Catalog No. T3623Alias XL518, RG7420, GDC-0973Cas No. 934660-93-2

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.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
2 mg	$47	In Stock	In Stock
5 mg	$77	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$183	In Stock	In Stock
50 mg	$291	In Stock	In Stock
100 mg	$477	In Stock	In Stock
500 mg	Inquiry	-	In Stock
1 mL x 10 mM (in DMSO)	$90	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.61%

Color:White

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COA LCMS HNMR

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]
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)
Synonyms	XL518, RG7420, GDC-0973

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

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

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc