PKM2-IN-6
Based on 1 publication(s) in Google Scholar
PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.
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- Pureté : 99.95%
- CAS No.: 771467-00-6
- Formule: C17H14N4OS
- Masse moléculaire:322.38
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PKM2-IN-6
More
Activité biologique
Description
IC50 & Target
IC50: 23 nM (PKM2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
14.38 μM
Compound: 7d
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Cytotoxicity against mouse 4T1 cells cultured as 2D cells assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
Cytotoxicity against mouse 4T1 cells cultured as 2D cells assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
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[PMID: 38408027] |
| 4T1 | IC50 |
23.27 μM
Compound: 7d
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Cytotoxicity against mouse 4T1 cells cultured as 3D tumor spheroids assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
Cytotoxicity against mouse 4T1 cells cultured as 3D tumor spheroids assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
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[PMID: 38408027] |
| A549 | IC50 |
47 μM
Compound: 7d
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Cytotoxicity against human A549 cells expressing PKM2 assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
Cytotoxicity against human A549 cells expressing PKM2 assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
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[PMID: 38408027] |
| COLO 205 | IC50 |
18.33 μM
Compound: 7d
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Cytotoxicity against human COLO 205 cells expressing PKM2 assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
Cytotoxicity against human COLO 205 cells expressing PKM2 assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
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[PMID: 38408027] |
| MCF7 | IC50 |
19.8 μM
Compound: 7d
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Cytotoxicity against human MCF7 cells expressing PKM2 assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
Cytotoxicity against human MCF7 cells expressing PKM2 assessed as inhibition of cell growth incubated for 48 hrs by alamar blue assay
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[PMID: 38408027] |
In Vitro
PKM2-IN-6 (compound 7d) (0, 20, 40, 60, 80, 100 μM; 48 h) shows cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively[1].
PKM2-IN-6 (14.38 μM; 48 h) induces apoptosis and cell cycle arrest at G2 phase[1].
PKM2-IN-6 (14.38 μM; 24 h) reduces the PKM1 and PKM2 at the mRNA level[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:COLO-205, A-549, MCF-7 cells
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Concentration:0, 20, 40, 60, 80, 100 μM
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Incubation Time:48 h
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Result:Showed cell cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively.
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Cell Line:4T1 cells
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Concentration:14.38 μM
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Incubation Time:24 h
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Result:Significantly reduced the level of PKM1 and PKM2 at the mRNA level.
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Cell Line:4T1 cells
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Concentration:14.38 μM
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Incubation Time:48 h
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Result:Induced apoptosis the percentage of live cells depreciated from 82.64% in control to 5.44% and the percentage of late apoptotic cells was 50.32% and necrotic cells were 44.08% in 2D culture; the difference is diminished as 89.05% of live cells in control dropped down to 52.45% and the percentage of late apoptotic cells was lesser (only 9.84%) and necrotic cells were 36.62% in 3D cell culture.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks, Female CD-1 nude mice (4T1-Red-FLuc cells)[1]
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Dosage:25, 50 mg/kg
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Administration:P.o.; daily for 3 weeks
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Result:Showed a significant regression in tumor volume and rendered significant reduction in tumor weight.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Real Time qPCR (Q-PCR)
Chemical Information
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CAS No. 771467-00-6
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Appearance Solid
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Masse moléculaire 322.38
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Formule C17H14N4OS
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Color Off-white to pink
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SMILES
COC1=CC=CC=C1NC2=NC(C3=CN=C4C=CC=CN43)=CS2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (310.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1019 mL | 15.5096 mL | 31.0193 mL | 77.5482 mL |
| 5 mM | 0.6204 mL | 3.1019 mL | 6.2039 mL | 15.5096 mL | |
| 10 mM | 0.3102 mL | 1.5510 mL | 3.1019 mL | 7.7548 mL | |
| 15 mM | 0.2068 mL | 1.0340 mL | 2.0680 mL | 5.1699 mL | |
| 20 mM | 0.1551 mL | 0.7755 mL | 1.5510 mL | 3.8774 mL | |
| 25 mM | 0.1241 mL | 0.6204 mL | 1.2408 mL | 3.1019 mL | |
| 30 mM | 0.1034 mL | 0.5170 mL | 1.0340 mL | 2.5849 mL | |
| 40 mM | 0.0775 mL | 0.3877 mL | 0.7755 mL | 1.9387 mL | |
| 50 mM | 0.0620 mL | 0.3102 mL | 0.6204 mL | 1.5510 mL | |
| 60 mM | 0.0517 mL | 0.2585 mL | 0.5170 mL | 1.2925 mL | |
| 80 mM | 0.0388 mL | 0.1939 mL | 0.3877 mL | 0.9694 mL | |
| 100 mM | 0.0310 mL | 0.1551 mL | 0.3102 mL | 0.7755 mL |
PKM2-IN-6 Related Classifications
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