| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Cereblon STAT3 19 nM (IC50); STAT1 270 nM (IC50); STAT5 >10 μM (IC50); STAT6 >10 μM (IC50)
|
|---|---|
| ln Vitro |
SD-436 inhibits the growth of MOLM-16 leukemia cell line, SU-DHL-1 and SUP-M2 lymphoma cell lines with IC50 values of 0.038 μM, 0.43 μM and 0.39 μM, respectively[1]. SD-436 (0.1 nM-40 μM, 20 h) can reduce the level of STAT3 protein in human PBMC, SU-DHL-1 and MOLM-16 cell lines[1]. SD-436 (0.1 nM-40 μM, 20 h) effectively reduces the level of mutant STAT3 (STAT3K658R) protein in Pfeiffer cell line in a dose-dependent manner with a DC50 value of 2.5 nM[1]. SD-436 shows excellent stability in mouse, rat, dog, monkey and human plasma with a T1/2 greater than 120 min[1]. SD-436 has no significant inhibitory effect on human ether-a-go-go potassium channels (hERG inhibition rate: 1.3% at 3 μM and 1.1% at 30 μM)[1].
|
| ln Vivo |
SD-436 (5 mg/kg, intravenous injection, single dose) can effectively induce rapid, complete and durable depletion of STAT3 in normal mouse tissues (liver and spleen) and MOLM-16 xenograft tumor tissues[1]. SD-436 (5-25 mg/kg, intravenous injection) shows antitumor activity in leukemia and lymphoma xenograft mouse models[1]. Pharmacokinetics of SD-436 in mice, rats, and dogs Species IV dose (mg/kg) t1/2 (h) Cmax (ng/mL) AUC(0-t) (h × ng/mL) Vz (L/kg) CI (mL/min/kg) Cl (%HBF) ICR mouse 5 22.1 130,185 859,223 0.10 0.051 0.1% SD rat 5 1.0 82,626 59,484 0.12 1.4 2.6% beagle dog 1 2.3 8861 10,699 0.29 1.5 2.7%
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: PBMC, MOLM-16, SU-DHL-1 and Pfeiffer Tested Tested Concentrations: 0.1 nM, 0.5 nM, 2.5 nM, 13 nM, 64 nM, 320 nM, 1600 nM, 8000 nM, 40000 nM Incubation Duration: 20 h Experimental Results: Reduced the levels of STAT3 protein in human PBMCs and SU-DHL-1 Cell Types, with DC50 of 0.1 nM and 10 nM, respectively. Achieved near complete degradation at 320 nM with merely a 4 h treatment time in the MOLM-16 Cell Types. Reduced the levels of the mutated STAT3 protein in a dose-dependent manner in the Pfeiffer Cell Types, with a DC50 value of 2.5 nM. Showed high selectivity for STAT3 over other STAT proteins. |
| Animal Protocol |
Animal/Disease Models: MOLM-16 acute leukemia xenograft model and the SU-DHL-1 lymphoma xenograft model in SCID mice (injected subcutaneously with 3 × 106 MOLM-16 cells or 5 × 106 SU-DHL-1 cells)[1]
Doses: 5, 10, 20 mg/kg (MOLM-16); 10, 25 mg/kg (SU-DHL-1) Route of Administration: Intravenous injection (i.v.); once a week, four weeks (MOLM-16: 5, 10, 20 mg/kg; SU-DHL-1: 10, 25 mg/kg) or twice a week, four weeks (SU-DHL-1: 25 mg/kg) Experimental Results: Showed that SD-436 at 5 mg/kg was able to achieve a maximum of 76% tumor regression in the MOLM-16 leukemia xenograft model. Induced complete tumor regression at 10 and 20 mg/kg in the MOLM-16 leukemia xenograft model. Achieved complete and long-lasting tumor regression in the SU-DHL-1 xenograft model at 25 mg/kg weekly dosing schedule. |
| References |
| Molecular Formula |
C58H62F4N9O14PS
|
|---|---|
| Molecular Weight |
1248.20
|
| CAS # |
2497585-50-7
|
| Appearance |
Typically exists as solids at room temperature
|
| 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 | 0.8012 mL | 4.0058 mL | 8.0115 mL | |
| 5 mM | 0.1602 mL | 0.8012 mL | 1.6023 mL | |
| 10 mM | 0.0801 mL | 0.4006 mL | 0.8012 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
