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Tunlametinib

Name: Tunlametinib
Brand: TargetMol
SKU: T39220
Price: 66 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T39220Cas No. 1801756-06-8

Alias HL-085, HL085

Tunlametinib is a highly selective, orally bioavailable small molecule inhibitor of MEK1 and MEK2 kinases with a reported IC50 value of 1.9 nM for MEK1. Tunlametinib exerts its antitumor effects by blocking the oncogenic RAS-RAF-MEK-ERK signaling pathway, thereby inducing tumor cell cycle arrest and promoting apoptosis, Tunlametinib demonstrates strong inhibitory activity against various RAS/RAF-mutant cancer cells such as those harboring BRAF V600E or KRAS G12C mutations, shows synergistic effects in combination with BRAF/KRASG12C/SHP2 inhibitors and Docetaxel, and is used in targeted therapy for RAS/RAF-driven cancers including melanoma, colorectal cancer, and non-small cell lung cancer (NSCLC).

Tunlametinib

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Purity: 98.72%

Catalog No. T39220Alias HL-085, HL085Cas No. 1801756-06-8

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$66	-	In Stock
5 mg	$158	-	In Stock
10 mg	$248	-	In Stock
25 mg	$397	-	In Stock
1 mL x 10 mM (in DMSO)	$173	-	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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Batch Information

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Purity:98.72%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Tunlametinib is a highly selective, orally bioavailable small molecule inhibitor of MEK1 and MEK2 kinases with a reported IC50 value of 1.9 nM for MEK1. Tunlametinib exerts its antitumor effects by blocking the oncogenic RAS-RAF-MEK-ERK signaling pathway, thereby inducing tumor cell cycle arrest and promoting apoptosis, Tunlametinib demonstrates strong inhibitory activity against various RAS/RAF-mutant cancer cells such as those harboring BRAF V600E or KRAS G12C mutations, shows synergistic effects in combination with BRAF/KRASG12C/SHP2 inhibitors and Docetaxel, and is used in targeted therapy for RAS/RAF-driven cancers including melanoma, colorectal cancer, and non-small cell lung cancer (NSCLC).
Targets&IC50	A549 cells:59.89 nM, HT-291 cells:10.07 nM, COLO 205 cells:0.94 nM, HL-60 cells:0.67 nM, Colo-829 cells:3.46 nM, A375 cells:0.86 nM
In vitro	Methods: A375 cells were treated with tunlametinib (1-9 nM, 48 h) to evaluate the effects on the cell cycle. Results: Tunlametinib increased the proportion of A375 cells in the G0/G1 phase in a dose-dependent manner and induced cell cycle arrest. Methods: Tunlametinib was used to treat BRAF/KRAS mutant cell lines: A375, Colo-829, HL-60 melanoma cells, COLO 205, HT-29 colon cancer cells, Calu-6, A549 lung cancer cells, and cell viability was determined by MTS assay. Results: The IC50 values of tunlametinib in the above cells were 0.86 nM, 3.46 nM, 0.67 nM, 0.94 nM, 10.07 nM, and 59.89 nM. [1]
In vivo	Methods: Tunlametinib (1, 3, 6 mg/kg, oral, once daily for 21 days) was used to treat female BALB/c nude mice, NU/NU mice, or Nod-Scid mice bearing A375 (BRAF V600E mutant melanoma), COLO 205 (BRAF V600E mutant colon cancer), and Calu-6 (KRAS Q61K mutant lung cancer) tumors, and the tumor growth in vivo was observed. Results: Tunlametinib inhibited tumor growth in the above mice in a concentration-dependent manner. [1]
Synonyms	HL-085, HL085

Chemical Properties

Molecular Weight	491.25
Formula	C₁₆H₁₂F₂IN₃O₃S
Cas No.	1801756-06-8
Smiles	O=C(NOCCO)C1=CC=2SC=NC2C(F)=C1NC3=CC=C(I)C=C3F
Relative Density.	no data available

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

DMSO: 80 mg/mL (162.85 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 5 mg/mL (10.18 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

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0356 mL	10.1781 mL	20.3562 mL	101.7812 mL
5 mM	0.4071 mL	2.0356 mL	4.0712 mL	20.3562 mL
10 mM	0.2036 mL	1.0178 mL	2.0356 mL	10.1781 mL
20 mM	0.1018 mL	0.5089 mL	1.0178 mL	5.0891 mL
50 mM	0.0407 mL	0.2036 mL	0.4071 mL	2.0356 mL
100 mM	0.0204 mL	0.1018 mL	0.2036 mL	1.0178 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