AK-1690
Based on 1 Customer Validation
AK-1690 is a selective PROTAC degrader targeting STAT6 (DC50=1 nM) with a Ki of 6 nM against human STAT6. AK-1690 degrades STAT6 via the interaction of STAT6 with cereblon and a ubiquitin-like process. AK-1690 effectively depletes STAT6 protein in mouse liver and lung tissues, and is applicable to research related to leukemia, Hodgkin's lymphoma, follicular lymphoma, etc..
(Pink: STAT6 ligand (HY-169182); Blue: Cereblon ligand (HY-131318); Black: linker (HY-W459522)).
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: 99.17%
- CAS 番号: 2984505-88-4
- 分子式: C51H56F2N5O11PS
- 分子量:1016.05
-
保管条件:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
PROTACs アイソフォーム固有の製品をすべて表示
More
生物活性
(Pink: STAT6 ligand (HY-169182); Blue: Cereblon ligand (HY-131318); Black: linker (HY-W459522)).
|
STAT6 1 nM (DC50) |
Cereblon |
AK-1690 potently induces STAT6 degradation in MV4;11 cells with a DC50 of 1 nM (12 h), and effectively induces STAT6 degradation in human peripheral blood mononuclear cells (PBMCs) with a DC50 of 80 nM (18 h)[1].
AK-1690 (0-10 μM; 24 h) effectively depletes total STAT6 and phosphorylated STAT6 in L1236 cells, with no impact on other STAT proteins even at concentrations as high as 10 μM[1].
AK-1690 (1 μM; 0-60 min, 120 min) exhibits excellent microsomal and plasma stability in humans, mice, rats, dogs, and monkeys, with a T1/2 value > 120 min (except for a T1/2 of 63 min in monkey microsomes)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:L1236 Hodgkin’s lymphoma cells (with activated STAT6)
-
Concentration:Up to 10 μM
-
Incubation Time:24 h
-
Result:Induced dose-dependent depletion of both total STAT6 and pSTAT6Y641 proteins; showed no effect on other STAT members up to 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Balb/c mouse model (female)[2]
-
Dosage:200 mg/kg
-
Administration:i.p.; single dose
-
Result:Depleted STAT6 by >90% in liver tissue at 2, 6, and 24 h time points; depleted STAT6 by >70%, >90%, and >70% in lung tissue at 2, 6, and 24 h time points, respectively.
化学情報
-
CAS 番号 2984505-88-4
-
性状 Solid
-
分子量 1016.05
-
分子式 C51H56F2N5O11PS
-
Color White to off-white
-
SMILES
FC(C1=CC=C2C(C=C(C(N[C@@H](C(C)(C)C)C(N3[C@H](C(N4C[C@@H](C5=CC=CC=C5)OCC4)=O)C[C@H](OCCCCCC#CC6=CC=CC7=C6CN(C(CC8)C(NC8=O)=O)C7=O)C3)=O)=O)S2)=C1)(P(O)(O)=O)F
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
DMSO : 100 mg/mL (98.42 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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)
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
純度とドキュメンテーション
-
データシート (277 KB)
-
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)
-
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 (protect from light, stored under nitrogen). 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 | 0.9842 mL | 4.9210 mL | 9.8420 mL | 24.6051 mL |
| 5 mM | 0.1968 mL | 0.9842 mL | 1.9684 mL | 4.9210 mL | |
| 10 mM | 0.0984 mL | 0.4921 mL | 0.9842 mL | 2.4605 mL | |
| 15 mM | 0.0656 mL | 0.3281 mL | 0.6561 mL | 1.6403 mL | |
| 20 mM | 0.0492 mL | 0.2461 mL | 0.4921 mL | 1.2303 mL | |
| 25 mM | 0.0394 mL | 0.1968 mL | 0.3937 mL | 0.9842 mL | |
| 30 mM | 0.0328 mL | 0.1640 mL | 0.3281 mL | 0.8202 mL | |
| 40 mM | 0.0246 mL | 0.1230 mL | 0.2461 mL | 0.6151 mL | |
| 50 mM | 0.0197 mL | 0.0984 mL | 0.1968 mL | 0.4921 mL | |
| 60 mM | 0.0164 mL | 0.0820 mL | 0.1640 mL | 0.4101 mL | |
| 80 mM | 0.0123 mL | 0.0615 mL | 0.1230 mL | 0.3076 mL |
AK-1690 関連分類
HY-169179 関連分類
Powered by Bioz