WS-691
WS-691 is an orally active, selective ABCB1 modulator. WS-691 selectively stabilizes ABCB1 via direct binding to ABCB1. WS-691 inhibits the efflux function of ABCB1 and activates ABCB1 ATPase activity. WS-691 elevates intracellular Paclitaxel (HY-B0015) levels and reduces the required dose of Paclitaxel in cancer cells overexpressing ABCB1. WS-691 increases the sensitivity of colon cancer cells to Paclitaxel.
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- CAS. Nr.: 2035417-32-2
- Formel: C20H16FN7S
- Molecular Weight:405.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI |
36.6 %
Compound: 6c
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Cytotoxicity against human A549 cells assessed as growth inhibition at 10 uM by MTT assay relative to control
Cytotoxicity against human A549 cells assessed as growth inhibition at 10 uM by MTT assay relative to control
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[PMID: 27769034] |
WS-691 (20 μM) reduces the IC50 of paclitaxel from 4.23 μM to 0.022 μM in paclitaxel-resistant cancer cells with ABCB1 overexpression, and exhibits no cytotoxicity when used alone[1].
WS-691 (0-40 μM; 20 min) stimulates the ATPase activity of ABCB1 to 2.5-fold of the basal activity[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 (male, 5-6 weeks old, 15-17 g, subcutaneous inoculation of SW620/Ad300 cells)[2]
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Dosage:20 mg/kg (single agent); 20 mg/kg (in combination with paclitaxel 5 mg/kg)
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Administration:i.g.; daily; 21 days;
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Result:Showed little effect on tumor growth compared to vehicle group when used as a single agent.
Significantly reduced tumor volume and tumor weight compared to paclitaxel alone, paclitaxel plus verapamil, or vehicle group when combined with paclitaxel.
Induced more tumor cell death (evident as nuclear pyknosis in HE staining) and higher levels of tumor cell apoptosis (evident as bright green staining in TUNEL assays) compared to single-agent and control groups when combined with paclitaxel.
Caused no obvious liver injury when used alone or in combination with paclitaxel.
Chemical Information
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CAS. Nr. 2035417-32-2
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Molecular Weight 405.45
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Formel C20H16FN7S
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SMILES
FC1=CC=C(NC2=CC(C)=NC3=NC(SCC4=NC5=C(N4)C=CC=C5)=NN32)C=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
Verweise
[1]. Abdelhafiz AHA, et al. Molecular design, synthesis and biological evaluation of novel 1,2,5-trisubstituted benzimidazole derivatives as cytotoxic agents endowed with ABCB1 inhibitory action to overcome multidrug resistance in cancer cells. J Enzyme Inhib Med Chem. 2022;37(1):2710-2724. [Content Brief]
[2]. Wang S, et al. Structure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-a]Pyrimidine Derivatives as Highly Potent and Orally Active ABCB1 Modulators. J Med Chem. 2020 Dec 24;63(24):15979-15996. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
WS-691 Related Classifications
HY-182253 Related Classifications
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