SD-436
Based on 1 Customer Validation
SD-436 is a highly selective and efficacious STAT3 PROTAC degrader (DC50: 0.5 μM), with IC50 of 19 nM (STAT3), 270 nM (STAT1), 360 nM (STAT4), >10 μM (STAT5) and >10 μM (STAT6). SD-436 promotes ubiquitination and degradation of STAT3, and induces tumor regression. SD-436 can be used for tumor research, such as leukemia and lymphoma.
(Pink: STAT3 ligand (HY-169361); Blue: Cereblon ligand (HY-43722); Black: linker (HY-147052)).
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.33%
- CAS No.: 2497585-50-7
- Formule: C58H62F4N9O14PS
- Masse moléculaire:1248.20
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Cereblon |
STAT3 19 nM (IC50) |
STAT1 270 nM (IC50) |
STAT5 >10 μM (IC50) |
STAT6 >10 μM (IC50) |
In Vitro
SD-436 (4 day treatment) inhibits the growth of MOLM-16 leukemia cell line, SU-DHL-1 and SUP-M2 lymphoma cell lines, with IC50 of 0.038 μM (MOLM-16), 0.43 μM (SU-DHL-1) and 0.39 μM (SUP-M2)[1].
SD-436 (0.1 nM-40 μM, 4 or 20 h) selectively reduces the levels of STAT3 protein in human PBMCs, SU-DHL-1 and MOLM-16 cell line (4 h)[1].
SD-436 (0.1 nM-40 μM, 20 h) effectively reduces the levels of the mutated STAT3 protein (STAT3K658R) in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM[1].
SD-436 shows excellent stability in mouse, rat, dog, monkey and human plasma, with T1/2 of >120 min[1].
SD-436 has no significant inhibition of the human ether-a-go-go-related gene potassium channels (hERG inhibition: 1.3% for 3μM and 1.1% for 30 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PBMC, MOLM-16, SU-DHL-1 and Pfeiffer
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Concentration:0.1 nM, 0.5 nM, 2.5 nM, 13 nM, 64 nM, 320 nM, 1600 nM, 8000 nM, 40000 nM
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Incubation Time:20 h
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Result:Reduced the levels of STAT3 protein in human PBMCs and SU-DHL-1 cell line, 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 line.
Reduced the levels of the mutated STAT3 protein in a dose-dependent manner in the Pfeiffer cell line, with a DC50 value of 2.5 nM.
Showed high selectivity for STAT3 over other STAT proteins.
In Vivo
SD-436 (5-25 mg/kg, i.v.) shows antitumor activity in leukemia and lymphoma xenograft models in mice[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% |
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (80.12 mM; Need ultrasonic; 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. 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. 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 (2.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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 (292 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. 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 |
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| DMSO | 1 mM | 0.8012 mL | 4.0058 mL | 8.0115 mL | 20.0288 mL |
| 5 mM | 0.1602 mL | 0.8012 mL | 1.6023 mL | 4.0058 mL | |
| 10 mM | 0.0801 mL | 0.4006 mL | 0.8012 mL | 2.0029 mL | |
| 15 mM | 0.0534 mL | 0.2671 mL | 0.5341 mL | 1.3353 mL | |
| 20 mM | 0.0401 mL | 0.2003 mL | 0.4006 mL | 1.0014 mL | |
| 25 mM | 0.0320 mL | 0.1602 mL | 0.3205 mL | 0.8012 mL | |
| 30 mM | 0.0267 mL | 0.1335 mL | 0.2671 mL | 0.6676 mL | |
| 40 mM | 0.0200 mL | 0.1001 mL | 0.2003 mL | 0.5007 mL | |
| 50 mM | 0.0160 mL | 0.0801 mL | 0.1602 mL | 0.4006 mL | |
| 60 mM | 0.0134 mL | 0.0668 mL | 0.1335 mL | 0.3338 mL | |
| 80 mM | 0.0100 mL | 0.0501 mL | 0.1001 mL | 0.2504 mL |
SD-436 Related Classifications
HY-169360 Related Classifications
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