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| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $68 | - | In Stock | |
| 5 mg | $168 | - | In Stock | |
| 10 mg | $272 | - | In Stock | |
| 25 mg | $542 | - | In Stock | |
| 50 mg | $868 | - | In Stock | |
| 100 mg | $1,390 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $185 | - | In Stock |
| Description | EV206 is a potent Hsp70 inhibitor, demonstrating significant anti-proliferative activity. This compound induces apoptosis and promotes increased protein expression of cleaved PARP and caspase-3, indicating its potential anti-tumor activity. |
| Targets & IC50 | SGC-7901 cells:0.27 μM, MGC-803 cells:0.06 μM, LoVo cells:1 μM, SW480 cells:0.38 μM, RKO cells:0.38 μM |
| In vitro | EV206 (1–10 μM; incubated for 30 minutes at 4°C) binds directly to the full-length Hsp70 protein and its N-terminal domain, but does not bind to the C-terminal domain [1]. In fluorescence-based equilibrium binding assays, EV206 (up to 250 μM; equilibrated at 20°C) exhibits a higher binding affinity for the N-terminal domain of Hsp70 (Kd = 16.60 μM) than for the C-terminal domain (Kd = 42.27 μM)[1]. EV206 (0.05–0.5 μM; 48 h) inhibits the viability of untreated H1299, A549, H460, H226B, and PC9 non-small cell lung cancer (NSCLC) cells; as determined by the crystal violet assay, the IC50 values were all below 0.5 μM after 48 h of treatment [1]. EV206 (0.05–0.5 μM; 2–3 weeks of culture) dose-dependently inhibited the adhesion-dependent colony formation of H1299, A549, H460, H226B, and PC9 non-small cell lung cancer (NSCLC) cells [1]. EV206 (0.1–0.5 μM; 48 h) induces apoptotic cell death in a dose-dependent manner in H1299, A549, H460, H226B, and PC9 non-small cell lung cancer (NSCLC) cells [1]. EV206 (0.1–0.5 μM; 48 h) dose-dependently reduces Hsp70 and Akt protein levels in H1299, A549, and H460 non-small cell lung cancer (NSCLC) cells, but does not affect Hsp90 protein levels [1]. EV206 (0.1–0.25 μM; 48 h) reduces the stability of Hsp70 protein in H460 non-small cell lung cancer cells via the ubiquitin-proteasome system, as confirmed by the reversal of Hsp70 downregulation following co-treatment with the proteasome inhibitor MG132 (treated at 10 μM for 6 h)[1]. EV206 (0.05–0.25 μM; 2–3 weeks of culture) dose-dependently inhibits the spheroid-forming ability of H1299, A549, and H460 non-small cell lung cancer (NSCLC) cells [1]. EV206 (0.05–0.25 μM; 48 h) reduces the activity of aldehyde dehydrogenase (ALDH) in H460 non-small cell lung cancer (NSCLC) cells; ALDH is a marker of the cancer stem cell (CSC)-like phenotype [1]. EV206 (0.1 μM during spheroid culture) significantly downregulates the mRNA expression of the cancer stem cell-associated markers POU5F1, NANOG, and SOX2 in H460 non-small cell lung cancer spheroids [1]. |
| In vivo | EV206 (10 mg/kg, administered intraperitoneally once every other day for 16 days) significantly inhibited the growth of H460 NSCLC xenografts in Balb/c nude mice without causing a detectable decrease in body weight [1]. |
| Molecular Weight | 329.40 |
| Formula | C21H19N3O |
| Cas No. | 2247047-81-8 |
| Smiles | O=C1C=2C=CC=CC2N(CC=C)C3C=4NC=5C=CC=CC5C4CCN13 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (121.43 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
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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