PF-6274484
Based on 1 Customer Validation
PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, 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: 98.76%
- CAS 番号: 1035638-91-5
- 分子式: C18H14ClFN4O2
- 分子量:372.78
-
保管条件:Powder -20°C, 3 years , 4°C, 2 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]
-
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
-
Immunology/Inflammation Compound Library
HY-L007
-
JAK/STAT Compound Library
HY-L008
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Covalent Screening Library
HY-L036
-
Differentiation Inducing Compound Library
HY-L038
-
Anti-Hepatitis C Virus Compound Library
HY-L073
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Obesity Compound Library
HY-L087
-
Angiogenesis-Related Compound Library
HY-L088
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Cysteine Targeted Covalent Library
HY-L153
-
Cytokine Inhibitors Library
HY-L161
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
EGFR アイソフォーム固有の製品をすべて表示
More
生物活性
|
EGFR (WT) 0.18 nM (Ki) |
EGFRL858R/T790M 0.14 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
1.6 μM
Compound: PF-6274484
|
Inhibition of PF-06422899 binding to recombinant C-terminal FLAG-tagged DUS2L (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay
Inhibition of PF-06422899 binding to recombinant C-terminal FLAG-tagged DUS2L (unknown origin) expressed in HEK293T cells after 1 hr by gel-based ABPP assay
|
[PMID: 28280261] |
化学情報
-
CAS 番号 1035638-91-5
-
性状 Solid
-
分子量 372.78
-
分子式 C18H14ClFN4O2
-
Color Light yellow to orange
-
SMILES
C=CC(NC1=CC2=C(NC3=CC(Cl)=C(F)C=C3)N=CN=C2C=C1OC)=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 25 mg/mL (67.06 mM; ultrasonic and warming and heat to 60°C; 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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (5.58 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 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:
-
-
-
-
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.
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 (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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. 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 | 2.6825 mL | 13.4127 mL | 26.8255 mL | 67.0637 mL |
| 5 mM | 0.5365 mL | 2.6825 mL | 5.3651 mL | 13.4127 mL | |
| 10 mM | 0.2683 mL | 1.3413 mL | 2.6825 mL | 6.7064 mL | |
| 15 mM | 0.1788 mL | 0.8942 mL | 1.7884 mL | 4.4709 mL | |
| 20 mM | 0.1341 mL | 0.6706 mL | 1.3413 mL | 3.3532 mL | |
| 25 mM | 0.1073 mL | 0.5365 mL | 1.0730 mL | 2.6825 mL | |
| 30 mM | 0.0894 mL | 0.4471 mL | 0.8942 mL | 2.2355 mL | |
| 40 mM | 0.0671 mL | 0.3353 mL | 0.6706 mL | 1.6766 mL | |
| 50 mM | 0.0537 mL | 0.2683 mL | 0.5365 mL | 1.3413 mL | |
| 60 mM | 0.0447 mL | 0.2235 mL | 0.4471 mL | 1.1177 mL |
PF-6274484 関連分類
HY-101450 関連分類
Powered by Bioz