EV206
Based on 1 Customer Validation
EV206 is a Hsp70 binder and apoptosis inducer that binds to the N-terminal domain of Hsp70, promotes Hsp70 degradation via the ubiquitin-proteasome system, and reduces Hsp70 protein stability. EV206 induces apoptotic cell death, inhibits colony formation, and downregulates the expression of cancer stem cell-related markers in non-small cell lung cancer cells. EV206 inhibits the growth of H460 xenograft tumors in nude mice and can be used for the research of non-small cell lung cancer.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.62%
- No. CAS: 2247047-81-8
- Fòrmula: C21H19N3O
- Peso molecular:329.40
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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HSP70 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HGC-27 | IC50 |
1.05 μM
Compound: 6k
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Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37099835] |
| LoVo | IC50 |
1 μM
Compound: 6k
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Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human LoVo cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37099835] |
| MGC-803 | IC50 |
0.06 μM
Compound: 6k
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Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37099835] |
| RKO | IC50 |
0.38 μM
Compound: 6k
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Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human RKO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37099835] |
| SGC-7901 | IC50 |
0.27 μM
Compound: 6k
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Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37099835] |
| SW480 | IC50 |
0.38 μM
Compound: 6k
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Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 37099835] |
EV206 (1-10 μM; 30 min at 4°C) binds directly to the full-length Hsp70 protein and its N-terminal domain, but not the C-terminal domain[1].
EV206 (up to 250 μM; equilibrated at 20°C) exhibits a higher binding affinity for the Hsp70 N-terminal domain (Kd = 16.60 μM) than for the C-terminal domain (Kd = 42.27 μM) in a fluorescence-based equilibrium binding assay[1].
EV206 (0.05-0.5 μM; 48 h) inhibits the viability of therapy-naïve H1299, A549, H460, H226B, and PC9 NSCLC cells with IC50 values below 0.5 μM after 48 h treatment, as measured by a crystal violet assay[1].
EV206 (0.05-0.5 μM; 48 h) inhibits the viability of drug-resistant H1299/CsR, H1299/PmR, H460/PcR, H226B/PcR, and PC9/ER NSCLC cells with IC50 values below 0.5 μM after 48 h treatment, as measured by a crystal violet assay[1].
EV206 (0.05-0.5 μM; 2-3 week culture) dose-dependently inhibits anchorage-dependent colony formation in H1299, A549, H460, H226B, and PC9 NSCLC cells[1].
EV206 (0.1-0.5 μM; 2-3 week culture) dose-dependently inhibits anchorage-independent colony formation in H1299, A549, H460, H226B, and PC9 NSCLC cells[1].
EV206 (0.1-0.5 μM; 48 h) dose-dependently induces apoptotic cell death (measured by increased sub-G1 population) in H1299, A549, H460, H226B, and PC9 NSCLC cells[1].
EV206 (0.1-0.5 μM; 48 h) dose-dependently induces apoptosis in H1299, A549, H460, H226B, and PC9 NSCLC cells, as shown by increased cleaved PARP and cleaved caspase-3 levels[1].
EV206 (0.1-0.5 μM; 48 h) dose-dependently reduces Hsp70 and Akt protein levels, but not Hsp90 protein levels, in H1299, A549, and H460 NSCLC cells[1].
EV206 (0.1-0.25 μM; 48 h) reduces Hsp70 protein stability in H460 NSCLC cells via the ubiquitin-proteasome system, as shown by the reversal of Hsp70 downregulation when co-treated with the proteasome inhibitor MG132 (10 μM for 6 h)[1].
EV206 (0.05-0.25 μM; 2-3 week culture) dose-dependently inhibits sphere formation (a marker of CSC-like phenotype) in H1299, A549, and H460 NSCLC cells[1].
EV206 (0.05-0.25 μM; 48 h) reduces aldehyde dehydrogenase (ALDH) activity, a marker of CSC-like phenotype, in H460 NSCLC cells[1].
EV206 (0.1 μM; during sphere culture) significantly downregulates the mRNA expression of CSC-associated markers POU5F1, NANOG, and SOX2 in H460 NSCLC spheres[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Therapy-naïve NSCLC cell lines (H1299, H460, A549, H226B, PC9)
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Concentration:0.05, 0.1, 0.5 μM
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Incubation Time:48 h
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Result:Potently inhibited cell viability across all tested therapy-naïve NSCLC cell lines, with IC50 values of 0.35 μM (H1299), 0.23 μM (A549), 0.31 μM (H460), 0.38 μM (H226B), and 0.46 μM (PC9).
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Cell Line:Drug-resistant NSCLC cell lines (H1299/CsR, H1299/PmR, H460/PcR, H226B/PcR, PC9/ER)
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Concentration:0.05, 0.1, 0.5 μM
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Incubation Time:48 h
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Result:Dose-dependently inhibited cell viability across all tested drug-resistant NSCLC cell lines, with IC50 values of 0.30 μM (H1299/CsR), 0.20 μM (H1299/PmR), 0.35 μM (H460/PcR), 0.30 μM (H226B/PcR), and 0.46 μM (PC9/ER).
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Cell Line:Therapy-naïve NSCLC cell lines (H1299, A549, H460, H226B, PC9)
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Concentration:0.05, 0.1, 0.5 μM
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Incubation Time:2-3 week culture
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Result:Dose-dependently suppressed colony formation in all tested therapy-naïve NSCLC cell lines, with significant inhibition observed at all tested concentrations.
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Cell Line:Therapy-naïve NSCLC cell lines (H1299, A549, H460, H226B, PC9)
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Concentration:0.1, 0.25, 0.5 μM
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Incubation Time:2-3 week culture
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Result:Dose-dependently suppressed soft agar colony formation in all tested therapy-naïve NSCLC cell lines, with significant inhibition observed at all tested concentrations.
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Cell Line:Therapy-naïve NSCLC cell lines (H1299, A549, H460)
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Concentration:0.1, 0.25, 0.5 μM
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Incubation Time:48 h
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Result:Dose-dependently decreased Hsp70 and Akt protein levels across all tested therapy-naïve NSCLC cell lines.
Did not alter Hsp90 protein levels across all tested therapy-naïve NSCLC cell lines.
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Cell Line:H460 NSCLC cells
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Concentration:0.1, 0.25 μM (EV206); 10 μM (MG132)
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Incubation Time:48 h (EV206); final 6 h (MG132)
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Result:Induced downregulation of Hsp70 protein levels in H460 cells.
Had this effect significantly blunted by co-treatment with MG132, indicating the effect is mediated via the ubiquitin-proteasome system.
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Cell Line:H460 NSCLC spheres
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Concentration:0.1 μM
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Incubation Time:during sphere culture
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Result:Caused a marked decrease in the mRNA expression of POU5F1 (Oct4), NANOG, and SOX2, all CSC-associated markers.
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 (6-week-old; male and female; H460 NSCLC xenograft model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every other day; 16 days
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Result:Inhibited H460 tumor xenograft growth.
Showed no significant changes in mouse body weight relative to vehicle controls.
Chemical Information
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No. CAS 2247047-81-8
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Appearance Solid
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Peso molecular 329.40
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Fòrmula C21H19N3O
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Color White to off-white
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SMILES
O=C1C2=C(C=CC=C2)N(CC=C)C(N1CC3)C4=C3C5=CC=CC=C5N4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (151.79 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)
Pureza y Documentación
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Ficha de datos (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.0358 mL | 15.1791 mL | 30.3582 mL | 75.8956 mL |
| 5 mM | 0.6072 mL | 3.0358 mL | 6.0716 mL | 15.1791 mL | |
| 10 mM | 0.3036 mL | 1.5179 mL | 3.0358 mL | 7.5896 mL | |
| 15 mM | 0.2024 mL | 1.0119 mL | 2.0239 mL | 5.0597 mL | |
| 20 mM | 0.1518 mL | 0.7590 mL | 1.5179 mL | 3.7948 mL | |
| 25 mM | 0.1214 mL | 0.6072 mL | 1.2143 mL | 3.0358 mL | |
| 30 mM | 0.1012 mL | 0.5060 mL | 1.0119 mL | 2.5299 mL | |
| 40 mM | 0.0759 mL | 0.3795 mL | 0.7590 mL | 1.8974 mL | |
| 50 mM | 0.0607 mL | 0.3036 mL | 0.6072 mL | 1.5179 mL | |
| 60 mM | 0.0506 mL | 0.2530 mL | 0.5060 mL | 1.2649 mL | |
| 80 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9487 mL | |
| 100 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.7590 mL |
EV206 Related Classifications
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