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TEPP-46

Name: TEPP-46
Brand: TargetMol
SKU: T7214
Price: 41 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7214Cas No. 1221186-53-3

Alias ML265

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.

TEPP-46

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Purity: 99.65%

Catalog No. T7214Alias ML265Cas No. 1221186-53-3

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$41	In Stock	In Stock
5 mg	$97	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$248	In Stock	In Stock
50 mg	$373	In Stock	In Stock
100 mg	$556	In Stock	In Stock
500 mg	$1,220	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$97	In Stock	In Stock

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

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Purity:99.65%

Color:White to Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.
Targets&IC50	PKM2:92 nM, C6 cells:81.8 μM, HCT116 cells:89.91 μM, A549 cells:> 100 μM, BxPC-3 cells:> 75 µM, MIAPaCa2 cells:> 75 µM
In vitro	METHODS: Human hepatocellular carcinoma cells, HepG2, were treated with TCEP hydrochloride (100-400 µM) for 3 days, and cell viability was measured by MTT assay. RESULTS: The viability of HepG2 was significantly reduced to 25.68% and 70.92% after treatment with 200 and 400 µM TCEP for 3 days, whereas the lowest concentration of TCEP (100 µM) did not significantly reduce the viability of HepG2 (3.44%). [1] METHODS: Human peripheral blood mononuclear cell PBMCs were treated with TCEP hydrochloride (0.5-1 mM) for 24 h. Morphological and necrotic changes were assessed by Hoechst 33342/PI staining. RESULTS: Necrosis was observed in cells treated with 0.5 mM of TCEP. [2]
In vivo	METHODS: To investigate the neurotoxicity and its mechanism in mice, TCEP hydrochloride (10-100 mg/kg) was administered by gavage to Kunming mice once a day for 30 days. RESULTS: Compared with the control group, the water intake of high-dose TCEP group was declined significantly, and the organ index of liver and spleen were increased significantly. In addition, the escape latency of TCEP exposed mice were longer than that in the control group in water maze test, while the total swimming course of high-dose TCEP group was elevated and the swimming time in target quadrant was obviously shortened compared with the control group. TCEP exposure can cause neurotoxicity by increasing thyroid hormones and inducing oxidative damage in mice. [3]
Synonyms	ML265

Chemical Properties

Molecular Weight	372.46
Formula	C₁₇H₁₆N₄O₂S₂
Cas No.	1221186-53-3
Smiles	Cn1c2cc(sc2c2cnn(Cc3cccc(N)c3)c(=O)c12)S(C)=O
Relative Density.	1.58 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 83.3 mg/mL (223.65 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.42 mM), Solution.

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	2.6849 mL	13.4243 mL	26.8485 mL	134.2426 mL
5 mM	0.5370 mL	2.6849 mL	5.3697 mL	26.8485 mL
10 mM	0.2685 mL	1.3424 mL	2.6849 mL	13.4243 mL
20 mM	0.1342 mL	0.6712 mL	1.3424 mL	6.7121 mL
50 mM	0.0537 mL	0.2685 mL	0.5370 mL	2.6849 mL
100 mM	0.0268 mL	0.1342 mL	0.2685 mL	1.3424 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