WHI-P258
Based on 1 Customer Validation
WHI-P258, a quinazoline compound, binds to the active site of JAK3 with an estimated Ki of 72 µM. WHI-P258 does not inhibit JAK3 and does not affect the thrombin-induced aggregation of platelets even at 100 μM.
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: 99.91%
- CAS 番号: 21561-09-1
- 分子式: C16H15N3O2
- 分子量:281.31
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
29 nM
Compound: 29
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Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles
Concentration required to inhibit the phosphorylation of a 14-residue fragment of phospholipase C gamma 1 by Epidermal growth factor receptor from A431 cell vesicles
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[PMID: 8568816] |
| A-431 | IC50 |
4.3 μM
Compound: 35
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Inhibition of human EGFR expressed in human A431 cells using poly(Glu4/Tyr) and [gamma32P]ATP as substrate after 1 hr by scintillation counting
Inhibition of human EGFR expressed in human A431 cells using poly(Glu4/Tyr) and [gamma32P]ATP as substrate after 1 hr by scintillation counting
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[PMID: 22229669] |
| MV4-11 | IC50 |
>1 nM
Compound: 1d
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Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
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[PMID: 30742435] |
化学情報
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CAS 番号 21561-09-1
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性状 Solid
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分子量 281.31
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分子式 C16H15N3O2
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Color White to off-white
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SMILES
COC1=CC2=NC=NC(NC3=CC=CC=C3)=C2C=C1OC
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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 In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
DMSO : 31.25 mg/mL (111.09 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.25 mg/mL (8.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.25 mg/mL (8.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Sudbeck EA, et al. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin Cancer Res. 1999 Jun;5(6):1569-82. [Content Brief]
[2]. Tibbles HE, et al. Role of a JAK3-dependent biochemical signaling pathway in platelet activation and aggregation. J Biol Chem. 2001 May 25;276(21):17815-22. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5548 mL | 17.7740 mL | 35.5480 mL | 88.8699 mL |
| 5 mM | 0.7110 mL | 3.5548 mL | 7.1096 mL | 17.7740 mL | |
| 10 mM | 0.3555 mL | 1.7774 mL | 3.5548 mL | 8.8870 mL | |
| 15 mM | 0.2370 mL | 1.1849 mL | 2.3699 mL | 5.9247 mL | |
| 20 mM | 0.1777 mL | 0.8887 mL | 1.7774 mL | 4.4435 mL | |
| 25 mM | 0.1422 mL | 0.7110 mL | 1.4219 mL | 3.5548 mL | |
| 30 mM | 0.1185 mL | 0.5925 mL | 1.1849 mL | 2.9623 mL | |
| 40 mM | 0.0889 mL | 0.4443 mL | 0.8887 mL | 2.2217 mL | |
| 50 mM | 0.0711 mL | 0.3555 mL | 0.7110 mL | 1.7774 mL | |
| 60 mM | 0.0592 mL | 0.2962 mL | 0.5925 mL | 1.4812 mL | |
| 80 mM | 0.0444 mL | 0.2222 mL | 0.4443 mL | 1.1109 mL | |
| 100 mM | 0.0355 mL | 0.1777 mL | 0.3555 mL | 0.8887 mL |
WHI-P258 関連分類
HY-108419 関連分類
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