| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SD-965 (maximum concentration 5 μM; incubation for 24 hours) effectively degraded STAT3 in the STAT3 HiBiT assay, with a half-maximal degradation concentration (DC50) of 0.14 μM and a maximum degradation rate of 85% after 24 hours of incubation [1]. SD-965 effectively inhibited the growth of MOLM-16 leukemia cells (IC50 = 1.3 nM) and SU-DHL-1 lymphoma cells (IC50 = 260 nM) [1]. SD-965 (concentration 3.2-2000 nM; incubation for 14 hours) selectively degraded STAT3 in human peripheral blood mononuclear cells (PBMCs), with a maximum degradation rate of over 90% after 14 hours of incubation, and had no significant effect on other STAT family proteins at concentrations up to 2 μM [1]. SD-965 exhibited excellent microsomal and plasma stability in mice, rats, dogs, monkeys and humans, with a half-life greater than 120 minutes in all tested matrices [1].
|
|---|---|
| ln Vivo |
SD-965 (25-50 mg/kg; intravenous injection; once a week; for 3-4 weeks) effectively inhibited tumor growth in a mouse model of SU-DHL-1 lymphoma xenograft[1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: SU-DHL-1 human degenerative large cell lymphoma cells Tested Concentrations: 3.2-2000 nM Incubation Duration: 14 hours Experimental Results: STAT3 was degraded with 80 nM DC50 and >90% Dₘₐₓ. No significant effect was observed on STAT1 or STAT6. STAT2 and STAT5 levels were slightly reduced at 2 μM, and STAT4 levels were increased in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:SU-DHL-1 lymphoma xenograft mouse model [1]
Doses: 25-50 mg/kg Route of Administration: Intravenous injection; once a week for 3-4 weeks Experimental Results: At a dose of 25 mg/kg, the tumor shrank by a maximum of 58%. On day 5 after the first administration, the tumor volume decreased by 52%, and on day 16 it decreased by 96%. 60% of the mice had no palpable tumor (50 mg/kg). |
| References |
| Molecular Formula |
C56H65N10O17PS
|
|---|---|
| Molecular Weight |
1213.21
|
| CAS # |
3054394-56-5
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(P(O)(O)=O)C1=CC2=C(NC(C(N[C@H]3CN(C(CCCCC(N4C[C@@]5([H])N(C6=C(OC5)C7=C(C(N([C@@H](CC8)C(NC8=O)=O)C7)=O)C=C6)CC4)=O)=O)CC[C@](CC[C@H]9C(N[C@@H](CCC(N)=O)COC%10=CC=CC(S(=O)(C)=O)=C%10)=O)([H])N9C3=O)=O)=C2)C=C1
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.8243 mL | 4.1213 mL | 8.2426 mL | |
| 5 mM | 0.1649 mL | 0.8243 mL | 1.6485 mL | |
| 10 mM | 0.0824 mL | 0.4121 mL | 0.8243 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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