YL-602
Based on 1 Customer Validation
YL-602 is an orally active Hippo pathway activator. YL-602 activates the Hippo pathway via MST1/2, with downstream pathway activation. YL-602 inhibits YAP and CTGF expression in cells irrespective of cell density and serum presence. YL-602 induces tumor cell apoptosis and inhibits colony formation. YL-602 suppresses tumor growth in mice. YL-602 can be used for the research of cancer, such as breast cancer.
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- Pureté : 99.76%
- CAS No.: 3081701-84-7
- Formule: C17H11NO4
- Masse moléculaire:293.27
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
[1]|
MST1 |
MST2 |
In Vitro
YL-602 (0.01-100 μM; 24 h) potently inhibits CTGF promoter activity in A549-CTGF cells with an EC50 of 0.474 μM[1].
YL-602 (0.62-10 μM; 24 h) activates the Hippo pathway in BxPC-3 and A549-CTGF cells by increasing phosphorylation of MST1/2, LATS1, and MOB1, reducing nuclear YAP localization, and decreasing total YAP and CTGF protein levels, without altering YAP/TAZ transcription[1].
YL-602 (1.25-20 μM; 12-14 days) potently inhibits colony formation in BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, and 4T1 cancer cells in a dose-dependent manner, but does not inhibit HT-29 cell colony formation at ≤10 μM[1].
YL-602 (2.5-20 μM; 5 days) induces dose-dependent apoptosis in BxPC-3 and MDA-MB-231 cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BxPC-3 cells, A549-CTGF cells
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Concentration:0.62, 1.25, 2.5. 5, 10 μM
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Incubation Time:24 h
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Result:Reduced nuclear YAP levels in BxPC-3 cells in a dose-dependent manner without altering YAP/TAZ mRNA levels.
Dose-dependently increased phosphorylation of MST1/2 (Thr183/Thr180), LATS1 (Thr1079), and MOB1 (Thr35) in both BxPC-3 and A549-CTGF cells, while leaving total MST1, LATS1, and MOB1 protein levels unchanged.
Reduced total YAP and CTGF protein levels in BxPC-3 cells.
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Cell Line:BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, 4T1, HT-29 cancer cells
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Concentration:1.25, 2.5. 5, 10, 20 μM
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Incubation Time:12-14 days
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Result:Dose-dependently inhibited colony formation in BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231, and 4T1 cells.
Achieved near-complete inhibition at 20 μM in BxPC-3 and SMMC-7721 cells.
Showed no significant inhibition in HT-29 cells at ≤10 μM.
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Cell Line:BxPC-3, MDA-MB-231 cancer cells
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Concentration:2.5. 5, 10, 20 μM
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Incubation Time:5 days
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Result:Induced early apoptosis in BxPC-3 cells in a dose-dependent manner and late apoptosis at 10-20 μM.
Induced apoptosis at 20 μM in MDA-MB-231 cells.
In Vivo
YL-602 (50 mg/kg; p.o.) significantly inhibits BXPC-3 pancreatic carcinoma tumor growth in nude mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 6 weeks old, 4T1 murine mammary carcinoma cells injected subcutaneously)[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 21 days
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Result:Reduced tumor volume and tumor weight in a dose-dependent manner.
Significantly decreased mean tumor weight at 100 mg/kg relative to vehicle control.
Increased phosphorylation levels of MST1/2, LATS1, and MOB1 in tumor tissues compared to vehicle control.
Decreased YAP protein levels in tumor tissues compared to vehicle control.
Caused no significant body weight loss or histopathological changes in heart, liver, spleen, lung, or kidney.
- RNA extraction experimental
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Breast Cancer Modeling
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Protocol for Cell Counting and Cell Density Analysis
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Soft Agar Colony Formation Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
Chemical Information
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CAS No. 3081701-84-7
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Appearance Solid
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Masse moléculaire 293.27
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Formule C17H11NO4
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Color Light yellow to yellow
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SMILES
C12=C3OCOC3=CC=C1C=C(C4=CC5=C(OCO5)C=C4)N=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 25 mg/mL (85.25 mM; Need warming; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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: ≥ 2.5 mg/mL (8.52 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (279 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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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 (sealed storage, away from moisture). 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 | 3.4098 mL | 17.0491 mL | 34.0983 mL | 85.2457 mL |
| 5 mM | 0.6820 mL | 3.4098 mL | 6.8197 mL | 17.0491 mL | |
| 10 mM | 0.3410 mL | 1.7049 mL | 3.4098 mL | 8.5246 mL | |
| 15 mM | 0.2273 mL | 1.1366 mL | 2.2732 mL | 5.6830 mL | |
| 20 mM | 0.1705 mL | 0.8525 mL | 1.7049 mL | 4.2623 mL | |
| 25 mM | 0.1364 mL | 0.6820 mL | 1.3639 mL | 3.4098 mL | |
| 30 mM | 0.1137 mL | 0.5683 mL | 1.1366 mL | 2.8415 mL | |
| 40 mM | 0.0852 mL | 0.4262 mL | 0.8525 mL | 2.1311 mL | |
| 50 mM | 0.0682 mL | 0.3410 mL | 0.6820 mL | 1.7049 mL | |
| 60 mM | 0.0568 mL | 0.2842 mL | 0.5683 mL | 1.4208 mL | |
| 80 mM | 0.0426 mL | 0.2131 mL | 0.4262 mL | 1.0656 mL |
YL-602 Related Classifications
HY-186148 Related Classifications
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