SD-91
Based on 1 Customer Validation
SD-91 (STAT3 degrader-2), a product of the hydrolysis of SD-36 (HY-129602), is a selective PROTAC-based STAT3 degrader with a Ki of 5.5 nM. SD-91 displays >300-fold selectivity over other STAT family protein members. SD-91 potently induces degradation of STAT3 protein in cells. SD-91 has anticancer effects, such as myeloid leukemia, lymphoma (Pink: ligand for target protein (HY-150895); Black: linker; Blue: E3 ligase ligand; E3 ligase ligand+linker: HY-176506).
(Pink: STAT3 ligand (HY-150895); Blue: E3 ligase ligand; Black: linker).
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- Reinheit : 97.49%
- CAS. Nr.: 2497583-03-4
- Formel: C59H62N9O13P
- Molecular Weight:1136.15
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
STAT3 5.5 nM (Ki) |
STAT3 28 nM (Kd) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| SU-DHL-1 | IC50 |
2.6 μM
Compound: SD-91; 2
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Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay
Antiproliferative activity against human SU-DHL-1 cells assessed as cell growth inhibition incubated for 4 days by CellTiter-Glo asssay
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[PMID: 34141084] |
In Vitro
SD-91 (Compound 92) (0.2 μM, 1 μM, 30 nM, 100 nM, 300 nM; 3 h) decreased the level of total STAT3 protein in acute leukemia Molm-16 cells[1].
In the BLI assays, SD-91 binds to STAT3 with a Kd value of 28 nM, while it displays a very weak affinity (Kd >10 μM) to all other STAT proteins (STAT1, STAT2, STAT4, STAT5A, STAT5B, and STAT6)[2].
In the MOLM-16 acute leukemia, SU-DHL-1, and SUP-M2 lymphoma cell lines, SD-91 has IC50 values of 0.17, 2.6, and 0.46 μM, respectively[2].
SD-91 (1-10 μM; 4 h) effectively reduce the levels of STAT3 protein in a dose-dependent manner, with DC50 values of 0.38 μM, 0.061μM, and 2.5 μM for MOLM-16, SU-DHL-1, and SUP-M2 cells, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Acute leukemia Molm-16 cells
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Concentration:0.2 μM, 1 μM; 30 nM, 100 nM, 300 nM
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Incubation Time:3 h
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Result:Degraded the level of total STAT3 protein in acute leukemia Molm-16 cells.
In Vivo
SD-91 (i.v.; 25, 50 mg/kg; qw) shows antitumor activity against Molm-16 xenograft tumors in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:25, 50 mg/kg
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Administration:i.v.; qw
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Result:Showed antitumor activity in Molm-16 and SU-DHL-1 xenograft mice.
Chemical Information
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CAS. Nr. 2497583-03-4
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Appearance Solid
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Molecular Weight 1136.15
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Formel C59H62N9O13P
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Color White to off-white
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SMILES
O=C(N1C[C@@H](C(N2[C@@](CC[C@H]2C(N[C@@H](CCC(N)=O)C(NC(C3=CC=CC=C3)C4=CC=CC=C4)=O)=O)([H])CC1)=O)NC(C5=CC6=CC(C(P(O)(O)=O)=O)=CC=C6N5)=O)CCCCCC#CC7=C8C(C(N(C9C(NC(CC9)=O)=O)C8)=O)=CC=C7
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Synonyms
STAT3 degrader-2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (88.02 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (277 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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Handling Instructions (2659 KB)
Verweise
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.8802 mL | 4.4008 mL | 8.8017 mL | 22.0041 mL |
| 5 mM | 0.1760 mL | 0.8802 mL | 1.7603 mL | 4.4008 mL | |
| 10 mM | 0.0880 mL | 0.4401 mL | 0.8802 mL | 2.2004 mL | |
| 15 mM | 0.0587 mL | 0.2934 mL | 0.5868 mL | 1.4669 mL | |
| 20 mM | 0.0440 mL | 0.2200 mL | 0.4401 mL | 1.1002 mL | |
| 25 mM | 0.0352 mL | 0.1760 mL | 0.3521 mL | 0.8802 mL | |
| 30 mM | 0.0293 mL | 0.1467 mL | 0.2934 mL | 0.7335 mL | |
| 40 mM | 0.0220 mL | 0.1100 mL | 0.2200 mL | 0.5501 mL | |
| 50 mM | 0.0176 mL | 0.0880 mL | 0.1760 mL | 0.4401 mL | |
| 60 mM | 0.0147 mL | 0.0733 mL | 0.1467 mL | 0.3667 mL | |
| 80 mM | 0.0110 mL | 0.0550 mL | 0.1100 mL | 0.2751 mL |
SD-91 Related Classifications
HY-150251 Related Classifications
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