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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 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 |
| 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]. |
| Molecular Weight | 322.38 |
| Formula | C17H14N4OS |
| Cas No. | 771467-00-6 |
| Smiles | N(C1=NC(C=2N3C(=NC2)C=CC=C3)=CS1)C4=C(OC)C=CC=C4 |
| Storage | keep 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
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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.
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.
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