| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PROTAC Sirt2 Degrader-2 (Compound W10) (72 hours) exhibited potent antiproliferative activity and high selectivity against a variety of ovarian cancer cell lines, including SKOV3 (IC50 = 0.33 μM), OVCAR3 (IC50 = 0.25 μM) and A2780 (IC50 = 0.08 μM) ovarian cancer cells, while showing low toxicity to normal cells IOSE80 (CC50 = 2.64 μM) [1]. PROTAC Sirt2 Degrader-2 (0.01-20 μM, 6-48 hours) can efficiently and selectively degrade SIRT2 protein in A2780 ovarian cancer cells. Its mechanism of action is concentration- and time-dependent, but a hook effect occurs at high concentrations [1]. PROTAC Sirt2 Degrader-2 (1 hour) can enhance the thermostability of SIRT2 protein in A2780 ovarian cancer cells, indicating that PROTAC Sirt2 Degrader-2 directly binds to SIRT2 and stabilizes its structure [1]. PROTAC Sirt2 Degrader-2 (0.01-5 μM, 14 days) inhibits the colony formation of A2780 cells in a concentration-dependent manner [1]. PROTAC Sirt2 Degrader-2 (0.01-10 μM, 36 hours) induces cell cycle arrest in A2780 cells during the S phase and G2/M phase [1]. PROTAC Sirt2 Degrader-2 (0.01-10 μM, 36 hours) induces early and late apoptosis in A2780 cells in a concentration-dependent manner, with late apoptosis being more significant [1].
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|---|---|
| ln Vivo |
PROTAC Sirt2 Degrader-2 (Compound W10) (3-10 mg/kg, intraperitoneal injection, every two days) can significantly inhibit the growth of A2780 tumor-bearing tumors without obvious toxicity and can effectively regulate the peripheral SIRT2 protein [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: A2780 ovarian cancer cells Tested Concentrations: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 20 μM Incubation Duration: 6 h, 9 h, 12 h, 24 h, 36 h, 48 h Experimental Results: Degradation was concentration-dependent (effective at 0.01 μmol/L, optimal at 1 μM, and exhibited a hook effect at 20 μM). Degradation was time-dependent (significant effect after 36 hours). Cell Cycle Analysis[1] Cell Types: A2780 ovarian cancer cells Tested Concentrations: 0.01 μM, 0.1 μM, 1 μM, 10 μM Incubation Duration: 36 h Experimental Results: Induced cell cycle arrest in A2780 cells during the S and G2/M phases. |
| Animal Protocol |
Animal/Disease Models: 5 × 106 cells human ovarian cancer cell line A2780 were injected subcutaneously into the right axillary region of female BALB/c nude mice (4 weeks old)[1].
Doses: 3 mg/kg, 5 mg/kg, 10 mg/kg Route of Administration: I.p., once every two days Experimental Results: Significantly inhibited the growth of ovarian cancer xenografts. Mice maintained stable body weight. Effectively degraded SIRT2 protein in vivo. The proportion of Ki-67 positive cells was significantly reduced, indicating that tumor cell proliferation was inhibited. |
| References |
| Molecular Formula |
C37H42N6O5S
|
|---|---|
| Molecular Weight |
682.83
|
| Appearance |
Typically exists as solids at room temperature
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| HS Tariff Code |
2934.99.9001
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| 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)
|
| 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 | 1.4645 mL | 7.3225 mL | 14.6449 mL | |
| 5 mM | 0.2929 mL | 1.4645 mL | 2.9290 mL | |
| 10 mM | 0.1464 mL | 0.7322 mL | 1.4645 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.
Products are for research use only; We do not sell to patients
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