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)).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.27%
- CAS 番号: 2497585-50-7
- 分子式: C58H62F4N9O14PS
- 分子量:1248.20
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
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Cereblon |
STAT3 19 nM (IC50) |
STAT1 270 nM (IC50) |
STAT5 >10 μM (IC50) |
STAT6 >10 μM (IC50) |
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.
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 |
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (292 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-169360 関連分類
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