| Size | Price | Stock | Qty |
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| Targets |
The target of MC-Val-Cit-PAB-retapamulin is the bacterial ribosome, specifically the 50S ribosomal subunit, where retapamulin inhibits bacterial protein synthesis. In the context of ADC applications, the conjugate is designed for targeted delivery to tumor cells or specific cell populations via antibody-mediated recognition. The MC-Val-Cit-PAB linker is cleavable by cathepsin B, an enzyme commonly overexpressed in the tumor microenvironment, enabling selective payload release.
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| ln Vitro |
MC-Val-Cit-PAB-retapamulin exhibits potent antitumor activity in vitro through the action of the retapamulin payload, which functions as a ribosome inhibitor. The conjugate demonstrates effective cell killing in ADC formats when paired with appropriate targeting antibodies. The MC-Val-Cit-PAB linker enables efficient intracellular release of the payload following antibody-mediated internalization and lysosomal processing. Standard purity is ≥98%.
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| ln Vivo |
In vivo, MC-Val-Cit-PAB-retapamulin demonstrates potent antitumor activity when incorporated into ADC constructs. The conjugate is designed to be stable in circulation while enabling targeted payload delivery to the tumor microenvironment. The MC-Val-Cit-PAB linker provides appropriate stability for systemic administration, with selective cleavage occurring within target cells. The retapamulin payload exerts its antiproliferative effects following intracellular release.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for MC-Val-Cit-PAB-retapamulin typically involve assessing the stability and cleavage characteristics of the linker-payload conjugate. 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. Ribosome binding assays may be performed to confirm the retained activity of the retapamulin payload.
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| Cell Assay |
In vitro cellular assays for MC-Val-Cit-PAB-retapamulin typically involve testing the conjugate in ADC formats using antigen-positive and antigen-negative cell lines. Cells are treated with varying concentrations (typically 0.001-100 nM range) of the ADC for 72-120 hours, and cell viability is assessed using standard assays such as MTT, CellTiter-Glo, or colony formation assays. Internalization and intracellular trafficking studies may be performed using fluorescently labeled constructs to confirm antibody-mediated uptake.
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| Animal Protocol |
In vivo animal studies for MC-Val-Cit-PAB-retapamulin ADC conjugates typically employ xenograft mouse models bearing human tumor cell lines. Tumor-bearing mice are administered the ADC via intravenous injection at various dose levels (typically 1-30 mg/kg) on schedules such as single dose or QD×5 or QW×2. Tumor growth inhibition is monitored over 2-4 weeks, with endpoints including tumor volume measurements, body weight monitoring, and survival analysis. Pharmacodynamic biomarkers may be assessed in tumor tissue.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MC-Val-Cit-PAB-retapamulin conjugates are characterized by typical ADC PK parameters. Following intravenous administration, the conjugate exhibits biphasic elimination with a distribution half-life and terminal half-life appropriate for antibody-based therapeutics. The linker-payload system provides stability in circulation, minimizing premature payload release. Standard PK assessments include measurement of total antibody, conjugate, and free payload concentrations in plasma via ELISA and LC-MS/MS methods.
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| Toxicity/Toxicokinetics |
Toxicological data for MC-Val-Cit-PAB-retapamulin is typical of ADC linker-payload constructs. The conjugate contains retapamulin, an antibiotic with established safety profiles. As a research reagent, standard safety precautions should be observed including appropriate PPE and fume hood use. Comprehensive toxicology studies including repeat-dose toxicity and genotoxicity assessments are typically conducted as part of ADC development programs but are not publicly available for this specific conjugate.
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| References | |
| Additional Infomation |
MC-Val-Cit-PAB-retapamulin is a research-grade drug-linker conjugate intended for ADC development and is not approved for clinical use. The compound is part of the emerging class of ADC payloads that repurpose antibiotics as cytotoxic agents. The MC-Val-Cit-PAB linker is a well-established ADC linker system that has been validated in multiple approved ADC products. This conjugate enables researchers to explore the utility of retapamulin as a payload for targeted cancer therapy. The compound is typically stored at -20degC under desiccated conditions.
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| Molecular Formula |
C58H86N7O10S
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|---|---|
| Molecular Weight |
1073.41
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| Exact Mass |
1107.584
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| CAS # |
1639793-15-9
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| PubChem CID |
170907798
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
24
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| Heavy Atom Count |
77
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| Complexity |
2190
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| Defined Atom Stereocenter Count |
12
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| SMILES |
[C@@]1([C@@H](O)[C@H](C)C23CC[C@@H](C)C([C@@]2(C(CC3)=O)[H])(C)[C@@H](C1)OC(=O)CS[C@@H]1C[C@@H]2[N+]([C@@H](CC2)C1)(CC1=CC=C(NC(=O)[C@H](CCCNC(=O)N)NC(=O)[C@H](C(C)C)NC(CCCCCN2C(=O)C=CC2=O)=O)C=C1)C)(C)C=C
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| InChi Key |
PLMIZWNAQGKFRQ-SZNIJRGJSA-N
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| InChi Code |
InChI=1S/C58H85N7O10S.ClH/c1-9-56(6)32-45(57(7)36(4)24-26-58(37(5)52(56)71)27-25-44(66)51(57)58)75-49(70)34-76-42-30-40-20-21-41(31-42)65(40,8)33-38-16-18-39(19-17-38)61-53(72)43(14-13-28-60-55(59)74)62-54(73)50(35(2)3)63-46(67)15-11-10-12-29-64-47(68)22-23-48(64)69;/h9,16-19,22-23,35-37,40-43,45,50-52,71H,1,10-15,20-21,24-34H2,2-8H3,(H5-,59,60,61,62,63,67,72,73,74);1H/t36-,37+,40-,41+,42?,43+,45-,50+,51+,52+,56-,57+,58+,65?;/m1./s1
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| Chemical Name |
[(1S,2R,3S,4S,6R,7R,8R,14R)-4-ethenyl-3-hydroxy-2,4,7,14-tetramethyl-9-oxo-6-tricyclo[5.4.3.01,8]tetradecanyl] 2-[[(1S,5R)-8-[[4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrol-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl]-8-methyl-8-azoniabicyclo[3.2.1]octan-3-yl]sulfanyl]acetate;chloride
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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 and light. |
| 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 : ~100 mg/mL (~90.18 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 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: 2.5 mg/mL (2.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9316 mL | 4.6581 mL | 9.3161 mL | |
| 5 mM | 0.1863 mL | 0.9316 mL | 1.8632 mL | |
| 10 mM | 0.0932 mL | 0.4658 mL | 0.9316 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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