Reagenti e strumenti per immunologia, biologia cellulare e biologia molecolare

K-975 [2563855-03-6]

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Cat# NB-64-46227-5mg

Size : 5mg

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K-975

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Synonyms:

Catalog No. T9954 Copy Product Info

Purity: 99.91%

K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.

Cas No. 2563855-03-6

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:99.91%

Appearance:Solid

Color:White

Product Introduction

Bioactivity

Description	K-975 is a highly selective, orally active TEAD inhibitor, effectively inhibiting protein-protein interactions between TEAD and YAP1/TAZ.
In vitro	K-975 inhibits the cell proliferation of NRF2-non-expressing malignant pleural mesothelioma (MPM) cell lines, protein-protein interaction (PPI) between Halo-TAZ and TEAD1/4 and Halo-YAP and endogenous TEAD1/4 in NCl-H226 cells and the reporter activity in NCl-H661/CTGF-Luc cells with the maximum of ~70%, at concentration of 0.1-10000 nM at 144 h and 24 h, respectively [1]. K-975 decreases the expression of IGFBP3, CTGF and NPPB mRNAs, and increases the expression of FBXO32 mRNA in NCl-H226 cells [1].
In vivo	K-975 (10-300 mg/kg; p.o. twice daily for 14 days) suppresses tumor growth by inhibiting TEAD-YAP1/TAZ signaling in MPM xenograft mouse models [1].

Chemical Properties

Molecular Weight	287.74
Formula	C₁₆H₁₄ClNO₂
Cas No.	2563855-03-6
Smiles	Cc1ccc(NC(=O)C=C)cc1Oc1ccc(Cl)cc1

Storage & Solubility Information

Storage

Store at low temperature,Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 140 mg/mL (486.55 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (34.75 mM), Suspension.

10% DMSO+90% Saline: < 10 mg/mL (34.75 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

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	3.4754 mL	17.3768 mL	34.7536 mL	173.7680 mL
5 mM	0.6951 mL	3.4754 mL	6.9507 mL	34.7536 mL
10 mM	0.3475 mL	1.7377 mL	3.4754 mL	17.3768 mL
20 mM	0.1738 mL	0.8688 mL	1.7377 mL	8.6884 mL
50 mM	0.0695 mL	0.3475 mL	0.6951 mL	3.4754 mL
100 mM	0.0348 mL	0.1738 mL	0.3475 mL	1.7377 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

Yes-associated proteinYAP1YAPTEAD,YAP1/TAZTEADTAZpleuralmesotheliomamalignantK-975K975K 975InhibitorinhibitCys359cancerantitumor

Related Tags: K-975 chemical structure | K-975 in vivo | K-975 in vitro | K-975 formula | K-975 molecular weight

K-975 [2563855-03-6]

Cat# NB-64-46227-5mg

Contatta il distributore locale :

Contatta il distributore locale :

K-975

Product Introduction

Calculator

In Vivo Formulation Calculator (Clear solution)

Dose Conversion

Keywords

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