| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
YL-602 (0.01-100 μM; 24 h) can effectively inhibit the activity of the CTGF promoter in A549-CTGF cells, with an EC50 of 0.474 μM[1]. YL-602 (0.62-10 μM; 24 h) can activate the Hippo pathway in BxPC-3 and A549-CTGF cells. The mechanism is to increase the phosphorylation of MST1/2, LATS1 and MOB1, reduce the nuclear localization of YAP, and reduce the total protein levels of YAP and CTGF without altering the transcription of YAP/TAZ[1]. YL-602 (1.25-20 μM; 12-14 days) effectively inhibited the colony formation of BxPC-3, MIA PaCa-2, SMMC-7721, MDA-MB-231 and 4T1 cancer cells in a dose-dependent manner, but did not inhibit the colony formation of HT-29 cells at ≤10 μM[1]. YL-602 (2.5-20 μM; 5 days) induced apoptosis in BxPC-3 and MDA-MB-231 cancer cells in a dose-dependent manner[1].
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|---|---|
| ln Vivo |
YL-602 (25-100 mg/kg; orally; daily; 21 days) significantly inhibited the growth of 4T1 breast cancer tumors in Balb/c mice by activating the Hippo pathway [1]. YL-602 (50 mg/kg; orally) significantly inhibited the growth of BXPC-3 pancreatic cancer tumors in nude mice [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: BxPC-3 cells, A549-CTGF cells Tested Concentrations: 0.62, 1.25, 2.5, 5, 10 μM Incubation Duration: 24 hours Experimental Results: In BxPC-3 cells, the nuclear YAP level decreased in a dose-dependent manner, but the YAP/TAZ mRNA level remained unchanged. In BxPC-3 and A549-CTGF cells, the phosphorylation levels of MST1/2 (Thr183/Thr180), LATS1 (Thr1079), and MOB1 (Thr35) increased in a dose-dependent manner, while the total protein levels of MST1, LATS1, and MOB1 remained unchanged. The total YAP and CTGF protein levels decreased in BxPC-3 cells. |
| Animal Protocol |
Animal/Disease Models:Balb/c (female, 6 weeks old, subcutaneously injected with 4T1 mouse breast cancer cells) [1]
Doses: 25 mg/kg; 50 mg/kg; 100 mg/kg Route of Administration: Oral; once daily; for 21 days Experimental Results: Tumor volume and tumor weight decreased in a dose-dependent manner. The mean tumor weight was significantly reduced in the 100 mg/kg dose group compared with the solvent control group. The phosphorylation levels of MST1/2, LATS1, and MOB1 in tumor tissue were increased compared with the solvent control group. The level of YAP protein in tumor tissue was decreased compared with the solvent control group. No significant weight loss or histopathological changes in the heart, liver, spleen, lungs, or kidneys were observed. |
| References |
| Molecular Formula |
C17H11NO4
|
|---|---|
| Molecular Weight |
293.27
|
| CAS # |
3081701-84-7
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
C12=C3OCOC3=CC=C1C=C(C4=CC5=C(OCO5)C=C4)N=C2
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4098 mL | 17.0491 mL | 34.0983 mL | |
| 5 mM | 0.6820 mL | 3.4098 mL | 6.8197 mL | |
| 10 mM | 0.3410 mL | 1.7049 mL | 3.4098 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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