SDUY212
SDUY212 is a TRPM7 inhibitor. SDUY212 attenuates EGF-induced STAT3 phosphorylation. SDUY212 induces Apoptosis and cell cycle arrest. SDUY212 exhibits anticancer activity against estrogen receptor-positive and triple-negative breast cancer.
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- Formel: C17H16ClN3
- Molecular Weight:297.78
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
SDUY212 is a TRPM7 inhibitor. SDUY212 attenuates EGF-induced STAT3 phosphorylation. SDUY212 induces Apoptosis and cell cycle arrest. SDUY212 exhibits anticancer activity against estrogen receptor-positive and triple-negative breast cancer[1].
IC50 & Target
[1]|
STAT3 |
TRPM7/ChaK1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.5 μM
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Inhibition of recombinant human TRPM7 currents in HEK293 cells assessed by whole-cell patch-clamp electrophysiology at +80 mV after extracellular application.
Inhibition of recombinant human TRPM7 currents in HEK293 cells assessed by whole-cell patch-clamp electrophysiology at +80 mV after extracellular application.
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42917899 |
| MDA-MB-231 | IC50 |
26 μM
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Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as viability reduction incubated 48 hrs by WST-8/CCK8 assay.
Antiproliferative activity against human MDA-MB-231 breast cancer cells assessed as viability reduction incubated 48 hrs by WST-8/CCK8 assay.
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42917899 |
| MCF7 | IC50 |
27 μM
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Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction incubated 48 hrs by WST-8/CCK8 assay.
Antiproliferative activity against human MCF-7 breast cancer cells assessed as viability reduction incubated 48 hrs by WST-8/CCK8 assay.
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42917899 |
In Vitro
Anti-cancerApoptosisCell Cycle RegulationCytokines & ChemokinesOthers
Anti-cancer
SDUY212 (5 μM) strongly inhibits native TRPM7 currents in U266 cells[1].
SDUY212 (20 μM; 12 h) directly engages and thermally stabilizes TRPM7 in MCF-7 cells, increasing Tm from 52.2 °C to 53.7 °C[1].
SDUY212 (10 μM; 48 h) inhibits MDA-MB-231 and MCF-7 proliferation with IC50 values of 26 μM and 27 μM, respectively[1].
SDUY212 (20 μM; 24 h) reduces wound-healing migration to 13% in MDA-MB-231 cells and 8% in MCF-7 cells[1].
SDUY212 (20 μM; 24 h) reduces invasion to 14% in MDA-MB-231 cells and suppresses invasion in MCF-7 cells[1].
SDUY212 (10-50 μM; 48 h) combined with BTP15 synergistically inhibits MCF-7 proliferation, with CI values below 0.75 at several tested combinations[1].
SDUY212 (20 μM; 12 h) directly engages and thermally stabilizes TRPM7 in MCF-7 cells, increasing Tm from 52.2 °C to 53.7 °C[1].
SDUY212 (10 μM; 48 h) inhibits MDA-MB-231 and MCF-7 proliferation with IC50 values of 26 μM and 27 μM, respectively[1].
SDUY212 (20 μM; 24 h) reduces wound-healing migration to 13% in MDA-MB-231 cells and 8% in MCF-7 cells[1].
SDUY212 (20 μM; 24 h) reduces invasion to 14% in MDA-MB-231 cells and suppresses invasion in MCF-7 cells[1].
SDUY212 (10-50 μM; 48 h) combined with BTP15 synergistically inhibits MCF-7 proliferation, with CI values below 0.75 at several tested combinations[1].
Anti-cancer
Apoptosis
Anti-cancer
Cell Cycle Regulation
SDUY212 (20 μM; 24 h) induces S-phase accumulation in MDA-MB-231 cells and G2/M arrest in MCF-7 cells[1].
Anti-cancer
Cytokines & Chemokines
Others
SDUY212 (0.3-5 μM; 140-340 s) potently inhibits recombinant hTRPM7 currents in HEK293 cells with an IC50 of 0.5 μM and 96% inhibition at 5 μM[1].
SDUY212 (5 μM) does not inhibit TRPM2 currents in HEK293 cells[1].
SDUY212 (5 μM) does not inhibit TRPM2 currents in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
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Cell Line:MDA-MB-231 and MCF-7 cells
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Concentration:10 μM (single-point antiproliferative activity); dose-response (IC50 determination)
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Incubation Time:48 h
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Result:At 10 μM, produced 61% antiproliferative activity in MDA-MB-231 cells and 49% in MCF-7 cells.
IC50 values were 26 μM in MDA-MB-231 cells and 27 μM in MCF-7 cells.
Cell Migration Assay [1]
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Cell Line:MDA-MB-231 and MCF-7 cells
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Concentration:10 and 20 μM
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Incubation Time:24 h
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Result:At 20 μM, reduced the migration ratio to 13% in MDA-MB-231 cells and to 8% in MCF-7 cells.
Cell Invasion Assay[1]
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Cell Line:MDA-MB-231 and MCF-7 cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:At 20 μM, reduced the invasion rate to 14% in MDA-MB-231 cells and markedly suppressed invasion in MCF-7 cells.
Apoptosis Analysis[1]
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Cell Line:MDA-MB-231 and MCF-7 cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:At 20 μM, induced apoptosis in 27% of MDA-MB-231 cells and 52% of MCF-7 cells.
Cell Cycle Analysis[1]
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Cell Line:MDA-MB-231 and MCF-7 cells
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Concentration:20 μM
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Incubation Time:24 h
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Result:In MDA-MB-231 cells, increased the S-phase fraction from 31% to 43% and decreased G0/G1 from 48% to 33%.
In MCF-7 cells, increased the G2/M fraction from 31% to 49% and decreased G0/G1 from 28% to 17%.
Western Blot Analysis[1]
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Cell Line:MCF-7 cells
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Concentration:3, 10, 30 μM
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Incubation Time:24 h
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Result:Inhibited EGF-induced STAT3 phosphorylation in a concentration-dependent manner, with reduced relative pSTAT3/STAT3 levels at increasing concentrations.
Cell Proliferation Assay[1]
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Cell Line:MCF-7 cells
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Concentration:10, 25, 50 μM (alone); 10, 25, 50 μM with BTP15 2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Alone at 10, 25, and 50 μM produced 28.0%, 40.0%, and 74.0% growth inhibition.
With BTP15 2.5 μM, 10, 25, and 50 μM produced 26.0%, 58.0%, and 89.0% inhibition; with BTP15 5 μM, 40.0%, 76.0%, and 92.0%; with BTP15 10 μM, 89.0%, 86.0%, and 100.0%.
CI values were 1.18, 0.88, and 0.85 with BTP15 2.5 μM; 1.07, 0.71, and 0.47 with BTP15 5 μM; and 0.74, 0.90, and 0.43 with BTP15 10 μM for 10, 25, and 50 μM, respectively.
Parmacokinetics
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUC | Clearance (CL) | Vss | Vz | F |
|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.08 h | 917 ng/mL | 0.50 h | 360 ng·h/mL | 2765 mL/h/kg | 927 mL/kg | / | / |
| Rat[1] | 10 mg/kg | p.o. | 0.5 h | 140 ng/mL | 1.57 h | 24 ng·h/mL | 41,854 mL/h/kg | / | 98,365 mL/kg | 7 % |
| Mice[1] | 3 mg/kg | i.v. | 0.08 h | 2720 ng/mL | 0.66 h | 1040 ng·h/mL | 2873 mL/h/kg | 986 mL/kg | / | / |
| Mice[1] | 6 mg/kg | i.v. | 0.08 h | 6997 ng/mL | 1.59 h | 2466 ng·h/mL | 2428 mL/h/kg | 890 mL/kg | / | / |
| Mice[1] | 6 mg/kg | p.o. | 0.25 h | 1393 ng/mL | 4.74 h | 1230 ng·h/mL | 4819 mL/h/kg | / | 32,929 mL/kg | 59 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, five-week-old)[1]
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Dosage:3 mg/kg and 6 mg/kg
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Administration:i.v.; once every 2 days; for 10 consecutive days
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Result:At 6 mg/kg, tumor growth inhibition (TGI) rate was 44.0%.
Excised tumor weights were substantially reduced relative to the vehicle control and NS8593 groups.
Related Protocols :
- Kinase activity and phosphorylation assays
- Western Blot
- 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
- Research Protocol for Endocrine Diseases
- Apoptosis Solutions
- Protocol for Cell Cycle
- Protocol for Kinase activity and phosphorylation assays
- Breast Cancer Modeling
Chemical Information
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Molecular Weight 297.78
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Formel C17H16ClN3
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SMILES
ClC1=CC=C2NC(N[C@@H]3CCCC4=C3C=CC=C4)=NC2=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Reinheit:
99.98%
Assay:
99.98%
ee.:
99.98%
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