| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
EGFR (Epidermal Growth Factor Receptor) protein tyrosine kinase. The peptide serves as a substrate for the EGFR kinase, mimicking the protein's phosphorylation target. It is not a drug that targets a biological entity but an analytical reagent.
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|---|---|
| ln Vitro |
As a peptide substrate, it does not have a defined "IC50." Its activity is measured by its ability to be phosphorylated by EGFR kinase in vitro. It is typically derived from the sequence of known EGFR substrates, such as the phosphorylation site in phospholipase C-gamma (PLCgamma) or other synthetic sequences.
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| ln Vivo |
No in vivo activity is applicable. The substrate is strictly an in vitro analytical reagent. Its use is to detect and quantify EGFR kinase activity in cell lysates or in purified enzyme systems, enabling the evaluation of potential EGFR inhibitors as part of drug discovery workflows.
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| Enzyme Assay |
The assay is cell-free and involves mixing the EGFR enzyme with ATP and the biotinylated EGFR peptide substrate. The reaction is performed in a multi-well plate. After incubation, the reaction mixture is transferred to a streptavidin-coated plate. Phosphorylation of the substrate is detected using a specific phospho-tyrosine antibody and a labeled secondary antibody.
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| Cell Assay |
Cell-based assays are not required for this substrate, as it is used directly in biochemical assays. Instead, cell lysates from cells treated with an EGFR inhibitor can be used as the source of EGFR enzyme, and the peptide substrate is added to the lysate to measure the kinase activity of the immunoprecipitated EGFR.
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| Animal Protocol |
No in vivo protocols exist for the substrate itself. For in vivo studies, an animal is dosed with an EGFR inhibitor. Tumor tissue is harvested and lysed. The EGFR enzyme is then immunoprecipitated from the lysate, and the kinase reaction is performed in vitro using the peptide substrate to measure the residual activity of the target.
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| ADME/Pharmacokinetics |
As a peptide, it is not a drug and has no pharmacokinetic parameters. It is supplied as a lyophilized solid (e.g., CAS 945830-38-6) and is reconstituted in a buffer solution for use in assays. It is stable in solution for short periods when stored on ice and is typically stored in aliquots at -20degC.
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| Toxicity/Toxicokinetics |
The EGFR Peptide Substrate is considered non-toxic for research purposes. Standard laboratory safety precautions for handling peptides should be followed, including avoiding inhalation and skin contact. It is not intended for human or veterinary use and has no therapeutic application.
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| Additional Infomation |
Other information: This substrate is an essential research tool for measuring EGFR kinase activity, which is a crucial parameter in drug discovery for cancer therapies. Its use allows for the rapid screening of potential EGFR inhibitors and the determination of inhibitor IC50 values in a high-throughput format. CAS number: 945830-38-6.
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| Molecular Formula |
C48H73N11O17
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|---|---|
| Molecular Weight |
1076.15673232079
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| Exact Mass |
1075.518
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| CAS # |
945830-38-6
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| PubChem CID |
162678811
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| Appearance |
White to off-white solid powder
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| LogP |
-4.5
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
76
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| Complexity |
2100
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C(N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@H](C(=O)O)CCC(=O)N)(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)C)CC1C=CC(O)=CC=1
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| InChi Key |
LQRUFPWSECMCHG-YBFBXAKBSA-N
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| InChi Code |
InChI=1S/C48H73N11O17/c1-6-24(4)39(47(74)59-19-7-8-34(59)46(73)53-28(13-16-35(50)61)41(68)54-30(48(75)76)14-17-36(51)62)58-45(72)31(20-23(2)3)56-43(70)32(21-26-9-11-27(60)12-10-26)57-42(69)29(15-18-37(63)64)52-44(71)33(22-38(65)66)55-40(67)25(5)49/h9-12,23-25,28-34,39,60H,6-8,13-22,49H2,1-5H3,(H2,50,61)(H2,51,62)(H,52,71)(H,53,73)(H,54,68)(H,55,67)(H,56,70)(H,57,69)(H,58,72)(H,63,64)(H,65,66)(H,75,76)/t24-,25-,28-,29-,30-,31-,32-,33-,34-,39-/m0/s1
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| Chemical Name |
(2S)-5-amino-2-[[(2S)-5-amino-2-[[(2S)-1-[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-5-oxopentanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 50 mg/mL (46.46 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (23.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9292 mL | 4.6461 mL | 9.2923 mL | |
| 5 mM | 0.1858 mL | 0.9292 mL | 1.8585 mL | |
| 10 mM | 0.0929 mL | 0.4646 mL | 0.9292 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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