VLS-1272
Based on 1 Customer Validation
VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CINHigh tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.63%
- CAS. Nr.: 2914878-00-3
- Formel: C27H35N3O5S2
- Molecular Weight:545.71
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 9.4 nM (KIF18A microtubule-dependent ATPase activity)[1]
In Vitro
VLS-1272 (Compound 22; 7 days) inhibits JIMT-1, NIH-OVCAR3 and HCC-15 cells viability with IC50s of 0.0078, 0.0097 and 0.011 μM, respectively[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:HCC-15, JIMT-1 and NIH-OVCAR3
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Concentration:
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Incubation Time:7 days
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Result:Inhibited cell viability with IC50s of 0.0078, 0.0097 and 0.011 μM against JIMT-1, NIH-OVCAR3 and HCC-15 cells, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID Beige mice, HCC15 tumor model[1]
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Dosage:10, 30 and 60 mg/kg
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Administration:PO, twice a day for 1 month
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Result:Inhibited tumor growth by 30±15%, 72±6% and 82±9% at 10, 30 and 60 mg/kg, respectively.
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Animal Model:Balb/C nude mice, OVCAR3 tumor model[1]
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Dosage:10, 30 and 60 mg/kg
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Administration:PO, once a day for 1 month
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Result:Inhibited tumor growth by 24±26%, 72±17% and 82±10% at 10, 30 and 60 mg/kg, respectively.
Chemical Information
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CAS. Nr. 2914878-00-3
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Appearance Solid
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Molecular Weight 545.71
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Formel C27H35N3O5S2
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Color White to off-white
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SMILES
O=S(C1=CC(C(N2CC3(CCC4(CC4)CC3)C5=CC(NS(C)(=O)=O)=CC=C52)=O)=CC=C1)(NC(C)(C)C)=O
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Synonyms
KIF18A-IN-7
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 25 mg/mL (45.81 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, 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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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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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Reinheit & Dokumentation
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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)
Verweise
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 |
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| DMSO | 1 mM | 1.8325 mL | 9.1624 mL | 18.3248 mL | 45.8119 mL |
| 5 mM | 0.3665 mL | 1.8325 mL | 3.6650 mL | 9.1624 mL | |
| 10 mM | 0.1832 mL | 0.9162 mL | 1.8325 mL | 4.5812 mL | |
| 15 mM | 0.1222 mL | 0.6108 mL | 1.2217 mL | 3.0541 mL | |
| 20 mM | 0.0916 mL | 0.4581 mL | 0.9162 mL | 2.2906 mL | |
| 25 mM | 0.0733 mL | 0.3665 mL | 0.7330 mL | 1.8325 mL | |
| 30 mM | 0.0611 mL | 0.3054 mL | 0.6108 mL | 1.5271 mL | |
| 40 mM | 0.0458 mL | 0.2291 mL | 0.4581 mL | 1.1453 mL |
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