| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
| Targets |
Fmoc-Phe-Lys(Boc)-PAB-PNP serves as an ADC linker, enabling the attachment of cytotoxic payloads to antibodies for targeted drug delivery. The Fmoc (9-fluorenylmethoxycarbonyl) group is a protecting group for solid-phase peptide synthesis. The Lys(Boc) provides a protected amine, and PAB-PNP enables conjugation to payloads.
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|---|---|
| ln Vitro |
Fmoc-Phe-Lys(Boc)-PAB-PNP is used as a cleavable ADC linker in the synthesis of antibody-drug conjugates. The linker is designed to be cleaved intracellularly, typically by cathepsin B, enabling targeted release of the payload within tumor cells. It is also used as a building block in solid-phase peptide synthesis (SPPS).
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| ln Vivo |
In vivo, Fmoc-Phe-Lys(Boc)-PAB-PNP is used in the synthesis of ADCs for targeted cancer therapy. The cleavable nature of the linker enables selective payload release within target cells, minimizing systemic toxicity. ADCs incorporating this linker are designed for stability in circulation and efficient payload delivery to tumors.
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| Enzyme Assay |
In vitro linker cleavage assays for Fmoc-Phe-Lys(Boc)-PAB-PNP typically involve assessing the stability and cleavage characteristics of the linker-payload construct. Cathepsin B-mediated release assays are performed by incubating the conjugate with recombinant cathepsin B at appropriate pH (typically 5.5) and temperature, followed by HPLC or LC-MS analysis to quantify payload release kinetics.
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| Cell Assay |
In vitro cellular assays for ADCs incorporating Fmoc-Phe-Lys(Boc)-PAB-PNP linkers involve treating antigen-positive and antigen-negative cell lines with varying concentrations of the ADC (typically 0.001-100 nM range) for 72-120 hours. Cell viability is assessed using standard assays such as MTT or CellTiter-Glo. Internalization studies confirm antibody-mediated uptake and intracellular payload release.
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| Animal Protocol |
In vivo animal studies for ADCs incorporating Fmoc-Phe-Lys(Boc)-PAB-PNP linkers typically employ xenograft mouse models bearing human tumor cell lines. Tumor-bearing mice are administered the ADC via intravenous injection at various dose levels. Tumor growth inhibition is monitored over 2-4 weeks. Endpoints include tumor volume, body weight, and survival.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ADCs incorporating Fmoc-Phe-Lys(Boc)-PAB-PNP linkers follow typical ADC PK profiles. Following intravenous administration, the conjugate shows biphasic elimination with stability in circulation. PK parameters including clearance, volume of distribution, and half-life are determined via ELISA for total antibody and conjugated antibody, and LC-MS/MS for free payload.
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| Toxicity/Toxicokinetics |
Fmoc-Phe-Lys(Boc)-PAB-PNP is a research-grade chemical for laboratory use only. As with all research chemicals, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. The compound is not intended for human therapeutic use. It is typically stored at 2-8degC.
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| Additional Infomation |
Fmoc-Phe-Lys(Boc)-PAB-PNP (CAS# 1646299-50-4) is a cleavable ADC linker used in the synthesis of antibody-drug conjugates. It is also used as a building block in solid-phase peptide synthesis. The compound is not approved for clinical use and is for research purposes only. It is typically stored at 2-8degC.
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| Molecular Formula |
C49H51N5O11
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|---|---|
| Molecular Weight |
885.956153154373
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| Exact Mass |
885.358
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| CAS # |
1646299-50-4
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| PubChem CID |
122403000
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| Appearance |
White to off-white solid powder
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| LogP |
8.6
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
65
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| Complexity |
1540
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)(C)OC(=O)NCCCC[C@@H](C(=O)NC1=CC=C(C=C1)COC(=O)OC2=CC=C(C=C2)[N+](=O)[O-])NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)OCC4C5=CC=CC=C5C6=CC=CC=C46
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| InChi Key |
AHKVECQGASADRU-MJPWBCPGSA-N
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| InChi Code |
InChI=1S/C49H51N5O11/c1-49(2,3)65-46(57)50-28-12-11-19-42(44(55)51-34-22-20-33(21-23-34)30-63-48(59)64-36-26-24-35(25-27-36)54(60)61)52-45(56)43(29-32-13-5-4-6-14-32)53-47(58)62-31-41-39-17-9-7-15-37(39)38-16-8-10-18-40(38)41/h4-10,13-18,20-27,41-43H,11-12,19,28-31H2,1-3H3,(H,50,57)(H,51,55)(H,52,56)(H,53,58)/t42-,43-/m0/s1
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| Chemical Name |
[4-[[(2S)-2-[[(2S)-2-(9H-fluoren-9-ylmethoxycarbonylamino)-3-phenylpropanoyl]amino]-6-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoyl]amino]phenyl]methyl (4-nitrophenyl) carbonate
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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 : ~6 mg/mL (~6.77 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 | 1.1287 mL | 5.6436 mL | 11.2872 mL | |
| 5 mM | 0.2257 mL | 1.1287 mL | 2.2574 mL | |
| 10 mM | 0.1129 mL | 0.5644 mL | 1.1287 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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