| Size | Price | Stock | Qty |
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| Targets |
Cleavable Linker
Fmoc-Gly-Gly-Phe-OtBu does not have a specific biological target as it is a synthetic linker for ADC development. Its role is to serve as a cleavable connector between an antibody and a cytotoxic payload in ADC synthesis. The Gly-Gly-Phe peptide sequence is designed for enzymatic cleavage by proteases such as cathepsin B, enabling targeted drug release within the tumor microenvironment. |
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| ln Vitro |
In vitro activity of Fmoc-Gly-Gly-Phe-OtBu is demonstrated by its utility as a cleavable ADC linker. The compound enables the synthesis of antibody-drug conjugates that exhibit potent cytotoxicity against target cancer cells. Its protease-sensitive peptide sequence allows for 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 Fmoc-Gly-Gly-Phe-OtBu 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, improving the therapeutic index.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not typically performed for Fmoc-Gly-Gly-Phe-OtBu as it is a linker, not a pharmacologically active compound. Its characterization involves assessing its purity, stability, and ability to form conjugates with drugs and antibodies. Cleavage assays using specific proteases such as cathepsin B can evaluate the linker's susceptibility to enzymatic degradation.
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| Cell Assay |
In vitro cellular assays for Fmoc-Gly-Gly-Phe-OtBu are conducted using ADCs synthesized with this linker. These assays evaluate the cytotoxicity of the resulting ADCs against target cancer cell lines. 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 Fmoc-Gly-Gly-Phe-OtBu 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 Fmoc-Gly-Gly-Phe-OtBu are typically derived from studies of ADCs synthesized using this linker. The compound has a molecular weight of 557.64. 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 Fmoc-Gly-Gly-Phe-OtBu 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 for research use only. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Bak A, et al. Synthesis and evaluation of the physicochemical properties of esterase-sensitive cyclic prodrugs of opioid peptides using an (acyloxy)alkoxy linker. J Pept Res. 1999 Apr;53(4):393-402.
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| Additional Infomation |
Fmoc-Gly-Gly-Phe-OtBu (CAS#: 236426-37-2) has the molecular formula C32H35N3O6 and a molecular weight of 557.64. It is a protected peptide ADC linker used in the synthesis of antibody-drug conjugates. The compound enables protease-sensitive drug release and site-specific antibody conjugation. It is for research use only.
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| Molecular Formula |
C32H35N3O6
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|---|---|
| Molecular Weight |
557.636808633804
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| Exact Mass |
557.252
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| CAS # |
236426-37-2
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| Related CAS # |
Fmoc-Gly-Gly-D-Phe-OtBu
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| PubChem CID |
11103667
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| Appearance |
White to off-white solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
41
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| Complexity |
890
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)(C)OC(=O)[C@H](CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)OCC2C3=CC=CC=C3C4=CC=CC=C24
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| InChi Key |
XQLGBXCTOOARCT-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C32H35N3O6/c1-32(2,3)41-30(38)27(17-21-11-5-4-6-12-21)35-29(37)19-33-28(36)18-34-31(39)40-20-26-24-15-9-7-13-22(24)23-14-8-10-16-25(23)26/h4-16,26-27H,17-20H2,1-3H3,(H,33,36)(H,34,39)(H,35,37)/t27-/m0/s1
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| Chemical Name |
tert-butyl (2S)-2-[[2-[[2-(9H-fluoren-9-ylmethoxycarbonylamino)acetyl]amino]acetyl]amino]-3-phenylpropanoate
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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 : 200 mg/mL (358.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (8.97 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (8.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7933 mL | 8.9664 mL | 17.9327 mL | |
| 5 mM | 0.3587 mL | 1.7933 mL | 3.5865 mL | |
| 10 mM | 0.1793 mL | 0.8966 mL | 1.7933 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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