EGFR Inhibitor (Synonyms: Epidermal Growth Factor Receptor Inhibitor) |
カタログ番号GC11312
One-Click Copy Product Info
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EGFR Inhibitor は 4,6-二置換ピリミジンであり、IC50 が 21 nM の強力な ATP 競合性、不可逆的かつ高度に選択的な EGFR 阻害剤です。 EGFR Inhibitor は、変異体 EGFRL858R および EGFRL861Q もそれぞれ 63 nM および 4 nM の IC50 で阻害します。 EGFR 阻害剤は、HER4 (IC50 = 7640 nM) および 55 の他のキナーゼのパネルよりも EGFR に対して強い選択性を示します。 EGFR阻害剤は、細胞のアポトーシスを誘導し、抗腫瘍活性を持っています。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 879127-07-8
Sample solution is provided at 25 µL, 10mM.
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EGFR inhibitor is a cell permeable, pyrimidine compound that selectively inhibits the EGFR kinase with IC50 value of 21 nM [1].
EGFR is a transmembrane protein, and is a receptor for members of epidermal growth factor family. The binding of EGFR with its ligands induces receptor dimerization and tyrosine autophosphorylation, and leads to cell proliferation. The overactivity of EGFR tyrosine kinases is associated with a number of cancers, inhibition of EGFR can downregulate antiapoptotic proteins such as surviving and upregulate proapoptotic proteins such as Bim. Thus, EGFR inhibitor can induce cell apoptosis, resulting in anti-tumor effectivity [2].
EGFR inhibitor inhibited EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR inhibitor also inhibited L858R and L861Q EGFR mutants with IC50 values of 63 and 4 nM, respectively [1].
References:
1. Q. Zhang, Y. Liu, F. Gao, et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. Journal of the American Chemical Society 128(7), 2182-2183 (2006).
2. F. Ciardiello, G. Tortora. EGFR antagonists in cancer treatment. New England Journal of Medicine 358(11), 1160-1174 (2008).
| Cas No. | 879127-07-8 | SDF | |
| 同義語 | Epidermal Growth Factor Receptor Inhibitor | ||
| Chemical Name | N-[3-[[6-[[3-(trifluoromethyl)phenyl]amino]-4-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide | ||
| Canonical SMILES | O=C(C1CC1)NC2=CC=CC(NC3=CC(NC4=CC(C(F)(F)F)=CC=C4)=NC=N3)=C2 | ||
| Formula | C21H18F3N5O | M.Wt | 413.4 |
| 溶解度 | ≤0.2mg/ml in ethanol;20mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.419 mL | 12.0948 mL | 24.1896 mL |
| 5 mM | 483.8 μL | 2.419 mL | 4.8379 mL |
| 10 mM | 241.9 μL | 1.2095 mL | 2.419 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)