DHFR-IN-4
Based on 1 Customer Validation
DHFR-IN-4 is a potent dihydrofolate reductase (DHFR) inhibitor with an IC50 value of 123 nM. DHFR-IN-4 also has inhibitory activity against EGFR and HER2 with IC50s of 246 nM and 357 nM, respectively. DHFR-IN-4 has remarkable broad spectrum cytotoxic potency against cancer cells.
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- Pureté : 99.19%
- CAS No.: 2820126-49-4
- Formule: C18H21N5O2S
- Masse moléculaire:371.46
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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
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Activité biologique
Description
IC50 & Target
IC50: 123 nM (DHFR), 246 nM (EGFR), 357 nM (HER2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
13.24 μM
Compound: 42
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Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells after 72 hrs by MTT assay
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[PMID: 35964425] |
| HeLa | IC50 |
6.9 μM
Compound: 42
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Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 35964425] |
| HepG2 | IC50 |
9.67 μM
Compound: 42
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Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
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[PMID: 35964425] |
| MCF7 | IC50 |
8.46 μM
Compound: 42
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Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
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[PMID: 35964425] |
| PC-3 | IC50 |
11.17 μM
Compound: 42
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Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC-3 cells after 72 hrs by MTT assay
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[PMID: 35964425] |
| WI-38 | IC50 |
89.61 μM
Compound: 42
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Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay
Antiproliferative activity against human WI-38 cells after 72 hrs by MTT assay
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[PMID: 35964425] |
In Vitro
DHFR-IN-4 (compound 42) (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency against HepG2, MCF-7, HCT-116, PC3 and HeLa[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:HepG2, MCF-7, HCT-116, PC3 and HeLa
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Concentration:0-100 μM
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Incubation Time:72 h
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Result:Exhibited antiproliferative activity against HepG2, MCF-7, HCT-116, PC3 and HeLa with IC50s of 9.67±0.7 μM, 8.46±0.7 μM, 13.24±0.9 μM, 11.17±1.0 μM and 6.90±0.5 μM.
Chemical Information
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CAS No. 2820126-49-4
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Appearance Solid
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Masse moléculaire 371.46
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Formule C18H21N5O2S
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Color White to off-white
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SMILES
O=C(C1=CSC2=NC(CN3CCOCC3)=C(C4=CC=C(C)C=C4)N21)NN
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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
Solvant et solubilité
In Vitro:
DMSO : 125 mg/mL (336.51 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)
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureté et documentation
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Fiche technique (278 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 | 2.6921 mL | 13.4604 mL | 26.9208 mL | 67.3020 mL |
| 5 mM | 0.5384 mL | 2.6921 mL | 5.3842 mL | 13.4604 mL | |
| 10 mM | 0.2692 mL | 1.3460 mL | 2.6921 mL | 6.7302 mL | |
| 15 mM | 0.1795 mL | 0.8974 mL | 1.7947 mL | 4.4868 mL | |
| 20 mM | 0.1346 mL | 0.6730 mL | 1.3460 mL | 3.3651 mL | |
| 25 mM | 0.1077 mL | 0.5384 mL | 1.0768 mL | 2.6921 mL | |
| 30 mM | 0.0897 mL | 0.4487 mL | 0.8974 mL | 2.2434 mL | |
| 40 mM | 0.0673 mL | 0.3365 mL | 0.6730 mL | 1.6825 mL | |
| 50 mM | 0.0538 mL | 0.2692 mL | 0.5384 mL | 1.3460 mL | |
| 60 mM | 0.0449 mL | 0.2243 mL | 0.4487 mL | 1.1217 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3365 mL | 0.8413 mL | |
| 100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6730 mL |
DHFR-IN-4 Related Classifications
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