| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Duostatin 5 functions as a cytotoxin in ADC applications, targeting cancer cells through antibody-mediated delivery. As a sea hare toxin analog, it exerts its cytotoxic effects by inhibiting tubulin polymerization, similar to other dolastatin derivatives. When conjugated to antibodies via ADC linkers, Duostatin 5 is selectively delivered to tumor cells, where it induces cell death. The compound's mechanism involves disruption of the microtubule cytoskeleton, leading to cell cycle arrest and apoptosis in target cancer cells.
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| ln Vitro |
Duostatin 5 demonstrates potent in vitro cytotoxic activity against cancer cell lines. As an ADC payload, its activity is typically assessed in cell viability assays using target-positive and target-negative cancer cell lines. The compound's potency is evaluated by measuring IC50 values in various cancer cell types. Duostatin 5 has been designed to serve as an effective cytotoxin in ADC applications. Its simple synthesis and stable chemical properties make it a valuable tool for ADC development and cancer research.
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| ln Vivo |
In vivo studies for Duostatin 5 are typically conducted as part of complete ADC development, where the antibody-drug conjugate is evaluated rather than the payload alone. The ADC containing Duostatin 5 is evaluated in mouse xenograft models bearing target-positive tumors. Efficacy is assessed by tumor growth inhibition, and pharmacokinetic studies evaluate the stability of the conjugate in circulation. The compound's in vivo performance depends on the specific antibody and linker used in the ADC construct.
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| Enzyme Assay |
For ADC synthesis, Duostatin 5 is conjugated to antibodies through appropriate linkers using standard bioconjugation techniques. The efficiency of conjugation is monitored by SDS-PAGE, mass spectrometry, or HPLC. For cytotoxicity assays, the ADC or Duostatin 5 alone is tested against cancer cell lines at various concentrations. Cell viability is measured using MTT, CellTiter-Glo, or similar assays. IC50 values are calculated from dose-response curves to assess the compound's potency and selectivity.
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| Cell Assay |
For cellular studies, target-positive and target-negative cancer cell lines are cultured in appropriate media and treated with Duostatin 5-containing ADCs or the payload alone at various concentrations. Cells are incubated for 48-72 hours, and cell viability is assessed using MTT or CellTiter-Glo assays. IC50 values are calculated to determine the compound's potency. Cell cycle analysis and apoptosis assays may be conducted to elucidate the mechanism of cell death. The specificity of the ADC is confirmed by comparing activity between target-positive and target-negative cell lines.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice bearing tumor xenografts are administered the Duostatin 5-containing ADC via intravenous injection. Dosing typically involves multiple injections at 1-2 week intervals. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity assessment. At study termination, tumors and major organs are collected for histopathological analysis and drug concentration measurement. Pharmacokinetic studies assess ADC stability and drug release in circulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Duostatin 5 are typically characterized as part of the complete ADC. The compound has a molecular weight of 772.03 and is soluble in DMSO at 100 mg/mL (129.53 mM). It should be stored under nitrogen, protected from direct sunlight, with powder stable at -20°C for 3 years and in solvent at -80°C for 1 year. In vivo formulation may use 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline at 4 mg/mL. Shipping is typically with blue ice or at ambient temperature.
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| Toxicity/Toxicokinetics |
Duostatin 5 is a research compound intended for laboratory use only and is not approved for human therapeutic use. As an ADC cytotoxin, it is designed to serve as an effective payload in antibody-drug conjugates. The compound has the advantages of fewer synthesis steps, easy operation, less difficulty in quality control, and a more stable chemical synthesis process. Standard laboratory safety precautions should be followed when handling this compound. It should be stored under nitrogen, protected from direct sunlight.
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| References | |
| Additional Infomation |
Duostatin 5 is a sea hare toxin analog (dolastatin derivative) used as a cytotoxin in ADC synthesis, with molecular formula C40H69N9O6 and molecular weight 772.03. It is designed based on MMAF and offers advantages including fewer synthetic steps, simple operation, and stable chemical synthesis. The compound is for research use only and has not been approved for clinical applications. Storage under nitrogen, protected from light, at -20°C for powder or -80°C for solvent is recommended.
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| Molecular Formula |
C40H69N9O6
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|---|---|
| Molecular Weight |
772.032569646835
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| Exact Mass |
771.537
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| CAS # |
2124210-34-8
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| PubChem CID |
138320017
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
55
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| Complexity |
1270
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| Defined Atom Stereocenter Count |
9
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| SMILES |
[C@@H]([C@]1([H])CCCN1C(=O)C[C@@H](OC)[C@H]([C@@H](C)CC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@@H](N(C)C)C(C)C)(OC)[C@@H](C)C(=O)N[C@H](CN=[N+]=[N-])CC1C=CC(N)=CC=1
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| InChi Key |
QIHHTRNUHMRKQK-MNFMTBGBSA-N
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| InChi Code |
InChI=1S/C40H69N9O6/c1-13-26(6)36(48(10)40(53)34(24(2)3)45-39(52)35(25(4)5)47(8)9)32(54-11)22-33(50)49-20-14-15-31(49)37(55-12)27(7)38(51)44-30(23-43-46-42)21-28-16-18-29(41)19-17-28/h16-19,24-27,30-32,34-37H,13-15,20-23,41H2,1-12H3,(H,44,51)(H,45,52)/t26-,27+,30-,31-,32+,34-,35-,36-,37+/m0/s1
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| Chemical Name |
(2S)-N-[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(2S)-1-(4-aminophenyl)-3-azidopropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-2-[[(2S)-2-(dimethylamino)-3-methylbutanoyl]amino]-N,3-dimethylbutanamide
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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: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). 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 : 125 mg/mL (161.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.69 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 20.8 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: ≥ 2.08 mg/mL (2.69 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 20.8 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 | 1.2953 mL | 6.4764 mL | 12.9529 mL | |
| 5 mM | 0.2591 mL | 1.2953 mL | 2.5906 mL | |
| 10 mM | 0.1295 mL | 0.6476 mL | 1.2953 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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