| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
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| 100mg |
|
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| Other Sizes |
| Targets |
PROTAC Linkers / ADC Linkers.
|
|---|---|
| ln Vitro |
As a linker molecule, this compound has no intrinsic biological activity; it serves as a peptide-based spacer that joins a payload to a targeting moiety in ADC or PROTAC applications. The tetrapeptide sequence enables cathepsin-mediated cleavage.
|
| ln Vivo |
No specific in vivo activity has been reported for this linker alone; its activity is derived from the complete conjugate (e.g., Deruxtecan ADC) after incorporation.
|
| Enzyme Assay |
N/A; this linker is not assessed in isolated enzyme binding assays but is used as a synthetic building block. Its peptide sequence is designed for specific enzymatic cleavage by cathepsins in the tumor microenvironment.
|
| Cell Assay |
N/A; this linker alone is not tested in cell-based assays but is incorporated into ADCs or PROTACs. The GGFG sequence is a valine-citrulline alternative that ensures stable circulation and controlled payload release.
|
| Animal Protocol |
N/A; no animal studies are performed with the linker alone. The pharmacokinetics and efficacy of the complete ADC conjugate are typically evaluated in xenograft models.
|
| ADME/Pharmacokinetics |
This peptide linker is designed for stability in circulation and selective cleavage by lysosomal cathepsins upon internalization into target cells. Typically stored as a powder at -20degC to maintain peptide integrity.
|
| Toxicity/Toxicokinetics |
This product is for laboratory research use only and is not for human therapeutic or clinical applications. Standard safety practices for handling peptide-based reagents should be followed.
|
| References |
[1]. NOGUCHI, Shigeru, et al. Method for selectively manufacturing antibody-drug conjugate. WO2017002776A1.
|
| Additional Infomation |
Fmoc protection allows for solid-phase peptide synthesis elongation, while the Cbz group protects the other terminus. Deruxtecan, containing this linker, is the payload component of FDA-approved ADCs such as Enhertu (fam-trastuzumab deruxtecan-nxki).
|
| Molecular Formula |
C40H41N5O9
|
|---|---|
| Molecular Weight |
735.781650304794
|
| Exact Mass |
735.29
|
| CAS # |
2264011-97-2
|
| Related CAS # |
Fmoc-Gly-Gly-(D-Phe)-Gly-CH2-O-CH2-Cbz
|
| PubChem CID |
148010663
|
| Appearance |
White to off-white solid
|
| LogP |
3.8
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
54
|
| Complexity |
1230
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
C(C1C2=CC=CC=C2C2=CC=CC=C12)OC(=O)NCC(=O)NCC(=O)N[C@H](C(=O)NCC(=O)NCOCC(=O)OCC1C=CC=CC=1)CC1C=CC=CC=1
|
| InChi Key |
IYTHCDKNSNAYJP-UMSFTDKQSA-N
|
| InChi Code |
InChI=1S/C40H41N5O9/c46-35(21-43-40(51)54-24-33-31-17-9-7-15-29(31)30-16-8-10-18-32(30)33)41-22-37(48)45-34(19-27-11-3-1-4-12-27)39(50)42-20-36(47)44-26-52-25-38(49)53-23-28-13-5-2-6-14-28/h1-18,33-34H,19-26H2,(H,41,46)(H,42,50)(H,43,51)(H,44,47)(H,45,48)/t34-/m0/s1
|
| Chemical Name |
benzyl 2-[[[2-[[(2S)-2-[[2-[[2-(9H-fluoren-9-ylmethoxycarbonylamino)acetyl]amino]acetyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]methoxy]acetate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~135.9 mM; with ultrasonication and warming by heating to 60°C)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3591 mL | 6.7955 mL | 13.5910 mL | |
| 5 mM | 0.2718 mL | 1.3591 mL | 2.7182 mL | |
| 10 mM | 0.1359 mL | 0.6796 mL | 1.3591 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.
Products are for research use only; We do not sell to patients
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