| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| 5g |
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| Other Sizes |
| Targets |
Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH targets the conjugation site between an antibody and a cytotoxic payload in ADC design. The linker does not have a direct biological target but serves as a cleavable connector that enables the selective delivery of cytotoxic agents to tumor cells expressing specific antigens. Its peptide sequence is designed for enzymatic cleavage, facilitating intracellular drug release.
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| ln Vitro |
In vitro activity of Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH is demonstrated by its ability to form stable drug-linker conjugates that can be conjugated to antibodies. The resulting ADCs exhibit potent cytotoxicity against target cancer cells. The linker's cleavable nature ensures efficient payload release upon internalization into target cells, contributing to the overall efficacy of the ADC.
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| ln Vivo |
In vivo activity of Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH is observed in the context of ADCs synthesized using this linker. These ADCs demonstrate targeted antitumor efficacy in animal models by delivering cytotoxic payloads specifically to tumor cells. The linker's design allows for stable circulation in the bloodstream followed by efficient payload release within the tumor microenvironment.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not typically performed for Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH as it is a linker, not a pharmacologically active compound. Its characterization involves assessing its stability, solubility, and ability to form conjugates with drugs and antibodies. Cleavage assays using specific enzymes (e.g., cathepsins) can evaluate the linker's susceptibility to enzymatic degradation.
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| Cell Assay |
In vitro cellular assays for Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH are conducted using ADCs synthesized with this linker. These assays evaluate the cytotoxicity of the resulting ADCs against target cancer cell lines expressing the relevant antigen. Cell viability is assessed using MTT or other assays, and IC50 values are determined to evaluate the potency of the ADC.
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| Animal Protocol |
In vivo animal experiments for Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH involve administering ADCs synthesized with this linker to tumor-bearing mouse models. Efficacy is evaluated by measuring tumor growth inhibition, survival rates, and body weight changes. The linker's performance is assessed based on the ADC's pharmacokinetic profile, stability, and antitumor activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH are typically derived from studies of ADCs synthesized using this linker. The linker influences the ADC's stability in circulation, clearance rate, and tissue distribution. The compound is designed to be stable in the bloodstream and to release the payload efficiently upon internalization into target cells.
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| Toxicity/Toxicokinetics |
Toxicological data for Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH are typically derived from studies of ADCs synthesized using this linker. The linker is designed to minimize systemic toxicity by ensuring targeted delivery of the cytotoxic payload to tumor cells. The compound is intended for research use only.
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| References | |
| Additional Infomation |
Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH (CAS#: 1599440-20-6) has the molecular formula C18H25N5O7 and a molecular weight of 423.42 g/mol. It is an ADC linker used for the synthesis of drug-linker conjugates, particularly for Deruxtecan. The compound is for research use only and is not for human therapeutic application.
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| Molecular Formula |
C18H25N5O7
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|---|---|
| Molecular Weight |
423.42
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| Exact Mass |
423.175
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| CAS # |
1599440-20-6
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| Related CAS # |
Gly-Gly-Phe-Gly-NH-CH2-O-CH2COOH;1599440-20-6
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| PubChem CID |
118305189
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| Appearance |
White to off-white solid powder
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| Density |
1.339±0.06 g/cm3(Predicted)
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| Boiling Point |
971.9±65.0 °C(Predicted)
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| LogP |
-4.1
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
30
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| Complexity |
608
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC=C(C=C1)C[C@@H](C(=O)NCC(=O)NCOCC(=O)O)NC(=O)CNC(=O)CN
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| InChi Key |
JKVPATHZQGMASP-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C18H25N5O7/c19-7-14(24)20-9-16(26)23-13(6-12-4-2-1-3-5-12)18(29)21-8-15(25)22-11-30-10-17(27)28/h1-5,13H,6-11,19H2,(H,20,24)(H,21,29)(H,22,25)(H,23,26)(H,27,28)/t13-/m0/s1
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| Chemical Name |
2-[[[2-[[(2S)-2-[[2-[(2-aminoacetyl)amino]acetyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]methoxy]acetic 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 (e.g. under nitrogen), 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) |
DMSO : 1 mg/mL (2.36 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3617 mL | 11.8086 mL | 23.6172 mL | |
| 5 mM | 0.4723 mL | 2.3617 mL | 4.7234 mL | |
| 10 mM | 0.2362 mL | 1.1809 mL | 2.3617 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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