Ki11502
Based on 1 Customer Validation
Ki11502 is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that selectively inhibits the activity of PDGF β/α receptors with IC50 values less than 10 nM. Ki11502 selectively inhibits PDGF β receptor phosphorylation, proliferation, and proteoglycan synthesis in human vascular smooth muscle cells. Ki11502 can induce Apoptosis) and exhibits profound antiproliferative effects on select subsets of leukemia, including those with Imatinib (HY-15463) resistant mutations. Ki11502 is highly suitable for studying the role of PDGF in vascular diseases, particularly the role of proteoglycans in atherosclerosis.
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: 99.30%
- CAS 番号: 347155-76-4
- 分子式: C26H23N3O4S
- 分子量:473.54
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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PDGFRα <10 nM (IC50) |
PDGFRβ <10 nM (IC50) |
KIT 86.81 nM (IC50) |
KIT670I 427.8 nM (IC50) |
FLT3 37.54 nM (IC50) |
FLT3D835Y 541.6 nM (IC50) |
KDR 210 nM (IC50) |
Ki11502 (0.1-1 nM; 2 days) significantly induces growth arrest, G0/G1 cell cycle arrest, and apoptosis in eosinophilic leukemia EOL-1 cells carrying the activated FIP1-like 1/PDGFRα fusion gene[2].
Ki11502 (0.1-1 nM; 3 h) effectively reduces the levels of p-PDGFRα and its downstream signals (including p-Akt, p-ERK, and p-STAT5) in EOL-1 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EOL-1, MOLM13, MV4-11
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Concentration:0.1 nM; 0.5 nM; 1 nM
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Incubation Time:48 h
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Result:Significantly downregulated the levels of Bcl-2, Bcl-xL, and Mcl-1 in EOL-1 cells, drastically reduced the level of Bcl-xL in MV4-11 cells, and notably decreased the expression of Mcl-1 in MOLM13 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 347155-76-4
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性状 Solid
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分子量 473.54
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分子式 C26H23N3O4S
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Color White to off-white
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SMILES
O=C(NC(NC1=CC=C(OC2=CC=NC3=CC(OC)=C(OC)C=C23)C=C1)=S)C4=CC=CC=C4C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 16.67 mg/mL (35.20 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)
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: ≥ 1.67 mg/mL (3.53 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
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.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (392 KB)
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- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Getachew R, et al. Characterisation of Ki11502 as a potent inhibitor of PDGF beta receptor-mediated proteoglycan synthesis in vascular smooth muscle cells. Eur J Pharmacol. 2010;626(2-3):186-192. [Content Brief]
[2]. Nishioka C, et al. Ki11502, a novel multitargeted receptor tyrosine kinase inhibitor, induces growth arrest and apoptosis of human leukemia cells in vitro and in vivo. Blood. 2008 May 15;111(10):5086-92. [Content Brief]
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 | 2.1118 mL | 10.5588 mL | 21.1175 mL | 52.7938 mL |
| 5 mM | 0.4224 mL | 2.1118 mL | 4.2235 mL | 10.5588 mL | |
| 10 mM | 0.2112 mL | 1.0559 mL | 2.1118 mL | 5.2794 mL | |
| 15 mM | 0.1408 mL | 0.7039 mL | 1.4078 mL | 3.5196 mL | |
| 20 mM | 0.1056 mL | 0.5279 mL | 1.0559 mL | 2.6397 mL | |
| 25 mM | 0.0845 mL | 0.4224 mL | 0.8447 mL | 2.1118 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7039 mL | 1.7598 mL |