SU4312
Based on 1 Customer Validation
SU4312 is the racemate of (Z)-SU4312 and (E)-SU4312. (Z)-SU4312 inhibits PDGFR and FLK-1 with IC50s of 19.4 and 0.8 μM, respectively. (E)-SU4312 inhibits PDGFR, FLK-1, EGFR, HER-2, and IGF-1R with IC50s of 24.2, 5.2, 18.5, 16.9 and 10.0 μM, respectively.
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: 99.74%
- CAS 番号: 5812-07-7
- 分子式: C17H16N2O
- 分子量:264.32
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保管条件:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
VEGFR 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
|
PDGFR |
Flk-1 |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
3.75 μM
Compound: 20, SU-4312
|
Inhibition of PDGFRbeta expressed in human A431 cells
Inhibition of PDGFRbeta expressed in human A431 cells
|
[PMID: 20558072] |
| SF-539 | IC50 |
3.7 μM
Compound: 22, DMBI
|
Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
|
[PMID: 23434139] |
| SF-539 | IC50 |
3.7 μM
Compound: 50, DMBI
|
Inhibition of PDGFRbeta phosphorylation in human SF539 cells after 10 mins by FLISA
Inhibition of PDGFRbeta phosphorylation in human SF539 cells after 10 mins by FLISA
|
[PMID: 20403700] |
| SF-539 | IC50 |
3.75 μM
Compound: 19, SU-4312
|
Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA
Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA
|
[PMID: 22739090] |
| SF-539 | IC50 |
3.75 μM
Compound: 21, DMBI
|
Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells after 60 mins by ELISA
Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells after 60 mins by ELISA
|
[PMID: 22204741] |
| SF-539 | IC50 |
3.75 μM
Compound: DMBI
|
Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine cell-based ELISA
Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine cell-based ELISA
|
[PMID: 20092323] |
| Sf9 | IC50 |
>100 μM
Compound: 43
|
Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells
Inhibition of human recombinant His-tagged RET expressed in Sf9 insect cells
|
[PMID: 20117004] |
Receptor tyrosine kinases (RTKs) have been shown to be important mediators of cellular signal transduction in cells. Many RTKs have been shown to be oncogene products implicating their role in the transformation process associated with human cancers[1].
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 5812-07-7
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性状 Solid
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分子量 264.32
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分子式 C17H16N2O
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Color Orange to red
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SMILES
O=C1NC2=C(C=CC=C2)/C1=C/C3=CC=C(N(C)C)C=C3
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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 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
溶剤 & 溶解度
DMSO : 50 mg/mL (189.16 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. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
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: 2.08 mg/mL (7.87 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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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-
-
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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. * The compound is unstable in solutions, freshly prepared is recommended.
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 (393 KB)
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- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7833 mL | 18.9165 mL | 37.8329 mL | 94.5823 mL |
| 5 mM | 0.7567 mL | 3.7833 mL | 7.5666 mL | 18.9165 mL | |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7833 mL | 9.4582 mL | |
| 15 mM | 0.2522 mL | 1.2611 mL | 2.5222 mL | 6.3055 mL | |
| 20 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7291 mL | |
| 25 mM | 0.1513 mL | 0.7567 mL | 1.5133 mL | 3.7833 mL | |
| 30 mM | 0.1261 mL | 0.6305 mL | 1.2611 mL | 3.1527 mL | |
| 40 mM | 0.0946 mL | 0.4729 mL | 0.9458 mL | 2.3646 mL | |
| 50 mM | 0.0757 mL | 0.3783 mL | 0.7567 mL | 1.8916 mL | |
| 60 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5764 mL | |
| 80 mM | 0.0473 mL | 0.2365 mL | 0.4729 mL | 1.1823 mL | |
| 100 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 mL |