ST6GAL1-IN-1
Based on 1 Customer Validation
ST6GAL1-IN-1 is an orally active selective ST6GAL1 inhibitor (IC50 = 20 μM). ST6GAL1-IN-1 exhibits high antimetastatic potential, effectively inhibiting the migration of MDA-MB-231 cells at noncytotoxic concentrations. ST6GAL1-IN-1 can disrupt integrin sialylation in MDA-MB-231 cells. ST6GAL1-IN-1 inhibits tumor angiogenesis and cancer metastasis via the Integrin/VEGFR2-mediated signaling pathway. ST6GAL1-IN-1 effectively suppresses both tumor growth and cancer metastasis on the MDA-MB-231 xenograft model. ST6GAL1-IN-1 can be used for the study of Triple-negative breast cancer (TNBC).
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- Pureté: 99.33%
- CAS No.: 192876-13-4
- Formule: C35H50N2O4
- Masse moléculaire:562.78
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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
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
12 μM
Compound: 20, PCM126
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Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA
Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA
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[PMID: 23489211] |
| PC-3 | IC50 |
5.1 μM
Compound: 20, PCM126
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Antagonist activity at EphA2 receptor in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated cell retraction pretreated for 15 mins by fluorescence microscopy
Antagonist activity at EphA2 receptor in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated cell retraction pretreated for 15 mins by fluorescence microscopy
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[PMID: 23489211] |
In Vitro
ST6GAL1-IN-1 (Compound 4e) (20-60 μM, 16 h) exhibits excellent antimigration properties, evident by its ability to hinder the migration of MDA-MB-231 cells even at noncytotoxic concentrations[1].
ST6GAL1-IN-1 (0.5-80 μM, 16 h) exhibits no observable cytotoxicity at concentrations between 0.5 and 20 μM in HUVEC cells, but it displayed cytotoxic effects beyond 40 μM[1].
ST6GAL1-IN-1 (10-40 μM, 16 h) can inhibit HUVEC tube formation in a dose-dependent manner[1].
ST6GAL1-IN-1 (10-40 μM, 5 days) inhibits ex vivo aortic ring formation in a dose-dependent manner[1].
ST6GAL1-IN-1 (0-80 μM) leads to a reduction in captured α-2,6-sialylated integrin subunits, with no observable effect towards α-2,3-sialylated integrin subunits in MDA-MB-231 Cells[1].
ST6GAL1-IN-1 (0-30 μM, 90 min) induces a dose-dependent repression of the phosphorylation of VEGFR2 at Tyr1175 and Akt at Ser473 while not affecting the overall expression of the wild-type proteins in MDA-MB-231 Cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0 μM, 20 μM, 40 μM, 60 μM
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Incubation Time:16 h
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Result:Effectively inhibited cancer cell migration at non-cytotoxic concentrations.
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Cell Line:MDA-MB-231 cells
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Concentration:0 μM, 20 μM, 40 μM, 80 μM
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Incubation Time:90 min
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Result:Dose-dependently inhibited the phosphorylation of VEGFR2 at Tyr1175 and Akt at Ser473 without affecting the total VEGFR2 and Akt protein levels.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The MDA-MB-231/Luc cells were dispersed in normal saline and injected subcutaneously into the Four- to five-week-old athymic nude mice’s (BALB/cAnN.Cg-Foxn1nu/CrlNarl) abdominal mammary gland region[1].
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Dosage:20 mg/kg, 40 mg/kg
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Administration:Oral gavage, once daily for 45 days
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Result:Effectively decreased tumor growth.
Detected Fewer metastatic nodules in lung specimens.
Chemical Information
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CAS No. 192876-13-4
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Appearance Solid
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Masse moléculaire 562.78
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Formule C35H50N2O4
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Color White to off-white
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SMILES
C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(N[C@H](C(O)=O)CC3=CNC4=CC=CC=C34)=O)([H])[C@@]5([H])[C@@](CC1)([H])[C@@]6([C@](C[C@@H](CC6)O)([H])CC5)C
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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 : 10 mg/mL (17.77 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (1.78 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (1.78 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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 | 1.7769 mL | 8.8845 mL | 17.7689 mL | 44.4223 mL |
| 5 mM | 0.3554 mL | 1.7769 mL | 3.5538 mL | 8.8845 mL | |
| 10 mM | 0.1777 mL | 0.8884 mL | 1.7769 mL | 4.4422 mL | |
| 15 mM | 0.1185 mL | 0.5923 mL | 1.1846 mL | 2.9615 mL |
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