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PKM2-IN-6

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Catalog No. T87217Cas No. 771467-00-6

PKM2-IN-6 (compound 7d) is an orally active PKM2 inhibitor (IC50=23 nM) capable of inducing apoptosis and G2 cell cycle arrest. It reduces PKM1 and PKM2 expression at the mRNA level, exhibits antitumour activity, and is suitable for investigating triple-negative breast cancer (TNBC).

PKM2-IN-6

PKM2-IN-6

🥰Excellent
Catalog No. T87217Cas No. 771467-00-6
PKM2-IN-6 (compound 7d) is an orally active PKM2 inhibitor (IC50=23 nM) capable of inducing apoptosis and G2 cell cycle arrest. It reduces PKM1 and PKM2 expression at the mRNA level, exhibits antitumour activity, and is suitable for investigating triple-negative breast cancer (TNBC).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$88-In Stock
5 mg$218-In Stock
10 mg$328-In Stock
25 mg$553-In Stock
50 mg$796-In Stock
100 mg$1,090-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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Product Introduction

Bioactivity
Description
PKM2-IN-6 (compound 7d) is an orally active PKM2 inhibitor (IC50=23 nM) capable of inducing apoptosis and G2 cell cycle arrest. It reduces PKM1 and PKM2 expression at the mRNA level, exhibits antitumour activity, and is suitable for investigating triple-negative breast cancer (TNBC).
In vitro
PKM2-IN-6 (compound 7d) (0-100 μM) exhibited cytotoxicity against COLO-205, A-549, and MCF-7 cells after 48 hours of treatment, with IC₅₀ values of 18.33 μM, 47.00 μM, and 19.80 μM, respectively [1].
PKM2-IN-6 (14.38 μM) induced apoptosis and caused cell cycle arrest at the G2 phase after 48 hours of treatment [1].
PKM2-IN-6 (14.38 μM) downregulated the expression of PKM1 and PKM2 at the mRNA level after 24 hours of treatment [1].
In vivo
PKM2-IN-6 (25 and 50 mg/kg, orally administered once daily for three weeks) significantly reduced tumor volume and weight in female CD-1 nude mice (6-8 weeks old) inoculated with 4T1-Red-FLuc cells [1].
Chemical Properties
Molecular Weight322.38
FormulaC17H14N4OS
Cas No.771467-00-6
SmilesN(C1=NC(C=2N3C(=NC2)C=CC=C3)=CS1)C4=C(OC)C=CC=C4
ColorYellow
AppearanceSolid
Storage & Solubility Information
Storagekeep away from moisture,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (310.19 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.1019 mL15.5096 mL31.0193 mL155.0965 mL
5 mM0.6204 mL3.1019 mL6.2039 mL31.0193 mL
10 mM0.3102 mL1.5510 mL3.1019 mL15.5096 mL
20 mM0.1551 mL0.7755 mL1.5510 mL7.7548 mL
50 mM0.0620 mL0.3102 mL0.6204 mL3.1019 mL
100 mM0.0310 mL0.1551 mL0.3102 mL1.5510 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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