K-975 [2563855-03-6]

Référence T9954-5mg

Conditionnement : 5mg

Marque : TargetMol

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K-975

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

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 Weight287.74
FormulaC16H14ClNO2
Cas No.2563855-03-6
SmilesCc1ccc(NC(=O)C=C)cc1Oc1ccc(Cl)cc1
Storage & Solubility Information
StorageStore 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
1mg5mg10mg50mg
1 mM3.4754 mL17.3768 mL34.7536 mL173.7680 mL
5 mM0.6951 mL3.4754 mL6.9507 mL34.7536 mL
10 mM0.3475 mL1.7377 mL3.4754 mL17.3768 mL
20 mM0.1738 mL0.8688 mL1.7377 mL8.6884 mL
50 mM0.0695 mL0.3475 mL0.6951 mL3.4754 mL
100 mM0.0348 mL0.1738 mL0.3475 mL1.7377 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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