ZW-1226
Based on 1 Customer Validation
ZW-1226 is a dual Tyrosyl DNA phosphodiesterase 2 (TDP2) and Multidrug resistance-associated protein 1 (MRP1) inhibitor with IC50 values of 0.2 and 0.5 μM, respectively. ZW-1226 exhibits selectivity over other ABC transporters. ZW-1226 elevates intracellular GSH levels, and reverses MRP1-mediated drug resistance. ZW-1226 can be used for the research of leukemia, non-small-cell lung cancer, and multidrug resistant small-cell lung cancer.
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- Purity: 98.13%
- CAS No.: 2351940-23-1
- 화학식: C25H16N4O3
- 분자량:420.42
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보관:
Store at room temperature, keep dry and cool.
In solvent -80°C, 1 year , -20°C, 6 months
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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Anti-Cancer Compound Library
HY-L025
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Blood Cancer Compound Library
HY-L079
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Cuproptosis Compound Library
HY-L133
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Cancer Stem Cells Compound Library
HY-L135
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Anti-Drug-Resistant Compound Library
HY-L169
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Anti-Hematopathy Compound Library
HY-L171
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Anti-Ovarian Cancer Compound Library
HY-L173
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | CC50 |
12 μM
Compound: 11a
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Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30998359] |
| HepG2 | CC50 |
14 μM
Compound: 11a
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 30998359] |
ZW-1226 (1-3 nM; 72 h) significantly reduces DT40 cell viability when combined with Etoposide (HY-13629) at 3 nM[1].
ZW-1226 (0.5-50 µM; 10 min) potently inhibits MRP1 with an IC50 of 0.5 µM in Sf9 cell membrane vesicles, with selectivity indices exceeding 100 over P-gp, BCRP, MRP2, and MRP3[2].
ZW-1226 (0.5-10 µM; 30 min) inhibits MRP1-mediated calcein efflux in H69AR cells with an IC50 of 0.5 µM, and this inhibitory effect is GSH-dependent[2].
ZW-1226 (5-50 µM; 5 min) inhibits substrate-stimulated MRP1 ATPase activity in Sf9 cell membrane vesicles, with no effect on baseline ATPase activity[2].
ZW-1226 (10 µM; 72 h) fully reverses MRP1-mediated resistance to Etoposide (ETP) (HY-13629) and Doxorubicin (DOX) (HY-15142A) in H69AR cells, without exhibiting intrinsic cytotoxicity[2].
ZW-1226 (1-10 µM; 1 h) increases elevates endogenous GSH levels in H69AR cells[2].
ZW-1226 binds preferentially to the LTC4-bound conformation of bovine MRP1, interacting with key residues near the H pocket, with binding enhanced by the presence of a GSH-containing substrate[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DT40 chicken lymphoma cells
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Concentration:1, 3 nM
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Incubation Time:72 h
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Result:decreased cell viability to 22% relative to vehicle control at 1 nM when combined with Etoposide.
Significantly decreased cell viability to less than 10% relative to vehicle control at 3 nM when combined with Etoposide.
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Cell Line:H69AR small-cell lung cancer cells, NCI-H69 cells
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Concentration:10 µM
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Incubation Time:72 h
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Result:Reduced the CC50 of ETP from 161.7 µM to 2.9 µM (56-fold reduction) in H69AR cells when co-treated at 10 µM.
Reduced the CC50 of DOX from 8.7 µM to 0.2 µM (44-fold reduction) in H69AR cells when co-treated at 10 µM.
Resulted in cell viability >90% in H69AR cells when used alone at 10 µM.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC | MRT | Vd | CL |
|---|---|---|---|---|---|---|---|---|---|
| Mice[2] | 4 mg/kg | i.p. | 228.4 min | 18.8 min | 411.3 nM | 38.0683 μM·min | 120.9 min | 79.3 L/kg | 0.22 L/min/kg |
Chemical Information
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CAS No. 2351940-23-1
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Appearance Solid
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분자량 420.42
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화학식 C25H16N4O3
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Color Light yellow to yellow
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SMILES
O=C(N=C1C2=CC3=C(C=C(C#N)C=C3)N1C4=CC=C(OCC5=CC=CC=C5)C=C4)NC2=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Store at room temperature, keep dry and cool
In solvent -80°C 1 year -20°C 6 months
용액&용해도
DMSO : 4 mg/mL (9.51 mM; ultrasonic and warming and heat to 60°C; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (280 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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Handling Instructions (2659 KB)
References
[1]. Belhadj Z, et al. Cancer sensitizing effect of deazaflavin analogs is associated with increased intracellular drug accumulation. Eur J Pharm Sci. 2024;193:106686. [Content Brief]
[2]. Belhadj Z, et al. Characterization of a deazaflavin analog as a potent inhibitor of multidrug resistance-associated protein 1. Biomed Pharmacother. 2024;178:117167. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3786 mL | 11.8929 mL | 23.7857 mL | 59.4643 mL |
| 5 mM | 0.4757 mL | 2.3786 mL | 4.7571 mL | 11.8929 mL |
ZW-1226 Related Classifications
HY-162753 Related Classifications
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