| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
Microtubule[1]
Auristatin F targets microtubules, specifically inhibiting tubulin polymerization. By binding to tubulin, it prevents the formation of microtubules, which are essential for mitotic spindle formation during cell division. This leads to cell cycle arrest in the G2/M phase and subsequent apoptosis in rapidly dividing cancer cells. It is a potent inhibitor of microtubule dynamics. |
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| ln Vitro |
In antibody-drug conjugates, Auristatin F and Monomethyl Auristatin F (MMAF) are strong ADC cytotoxins[1].
In vitro, Auristatin F is a potent microtubule inhibitor and vascular damaging agent. It stops tubulin from aggregating, which stops cell division. It is a strong cytotoxin used in antibody-drug conjugates (ADCs). Its cytotoxicity has been characterized in various cancer cell lines. Auristatin F and Monomethyl Auristatin F (MMAF) are strong ADC cytotoxins. |
| ln Vivo |
8276.76 ng/mL is the Cmax of auristatin F (5 mg/kg; i.v.; male Sprague-Dawley rats). The clearance (CL) is 77.33 mL/min/kg, which is higher than the rat's hepatic blood flow, and the AUClast is 65661.30 min*ng/mL[2].
In vivo, Auristatin F has been studied in pharmacokinetic studies in male Sprague-Dawley rats. At a dose of 5 mg/kg (i.v.), the Cmax was 8276.76 ng/mL, the clearance (CL) was 77.33 mL/min/kg (higher than the rat's hepatic blood flow), and the AUClast was 65661.30 min*ng/mL. As an ADC payload, its in vivo efficacy and toxicity are dependent on the targeting antibody and linker used. |
| Enzyme Assay |
The activity of Auristatin F can be assessed using cell-free tubulin polymerization assays. Tubulin is incubated with varying concentrations of Auristatin F, and the extent of polymerization is measured spectrophotometrically by monitoring the increase in turbidity. The IC₅₀ for inhibition of tubulin polymerization is determined from dose-response curves.
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| Cell Assay |
To evaluate the cellular effects of Auristatin F, cancer cells are treated with the compound. Cell viability, proliferation, and cell cycle distribution are assessed using standard assays such as MTT, BrdU incorporation, and flow cytometry. The effects on microtubule organization are visualized by immunofluorescence microscopy using anti-tubulin antibodies. Apoptosis is measured using Annexin V/PI staining or caspase activity assays.
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| Animal Protocol |
Animal Model: Male Sprague-Dawley rats[2]
Dosage: 5 mg/kg Administration: Intravenous injection In vivo studies with Auristatin F typically involve its use as a payload in antibody-drug conjugates (ADCs). The ADC is administered to tumor-bearing mice, and its effects on tumor growth, survival, and toxicity are assessed. The pharmacokinetics and biodistribution of the ADC and released Auristatin F are characterized. In some cases, the free drug may be studied in toxicology models. |
| ADME/Pharmacokinetics |
Auristatin F has a molecular formula of C₄₀H₆₇N₅O₈ and a molecular weight of 746.003 g/mol. Its CAS number is 163768-50-1. It appears as an off-white to yellow solid powder with a density of 1.1±0.1 g/cm³. It has a logP of 4.99. It is soluble in DMSO. The purity is typically ≥98%.
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| Toxicity/Toxicokinetics |
Auristatin F is a potent cytotoxin and should be handled with extreme caution. As a microtubule inhibitor, it can cause severe toxicity in rapidly dividing cells. It is intended for research use only and is not for human consumption. When used in ADCs, its toxicity is targeted to tumor cells, but off-target effects can still occur.
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| References |
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| Additional Infomation |
Auristatin F is a potent microtubule inhibitor and a member of the auristatin family of cytotoxic compounds. It is an MMAF analog used as a payload in antibody-drug conjugates (ADCs) for targeted cancer therapy. Auristatin F prevents tubulin polymerization, arresting cell division and inducing apoptosis in cancer cells. It is a valuable research tool for studying microtubule dynamics and developing ADC-based therapeutics.
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| Molecular Formula |
C40H67N5O8
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|---|---|
| Molecular Weight |
746.003
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| Exact Mass |
745.498
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| Elemental Analysis |
C, 64.40; H, 9.05; N, 9.39; O, 17.16
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| CAS # |
163768-50-1
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| Related CAS # |
Auristatin F-d8
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| PubChem CID |
67472795
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
894.4±65.0 °C at 760 mmHg
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| Flash Point |
494.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.523
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| LogP |
4.99
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
53
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| Complexity |
1190
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(C)[C@H](N(C)C)C(N[C@H](C(N([C@@H]([C@@H](C)CC)[C@@H](CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(N[C@H](C(O)=O)CC2=CC=CC=C2)=O)=O)OC)C)=O)C(C)C)=O
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| InChi Key |
LGNCNVVZCUVPOT-FUVGGWJZSA-N
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| InChi Code |
InChI=1S/C40H67N5O8/c1-13-26(6)35(44(10)39(49)33(24(2)3)42-38(48)34(25(4)5)43(8)9)31(52-11)23-32(46)45-21-17-20-30(45)36(53-12)27(7)37(47)41-29(40(50)51)22-28-18-15-14-16-19-28/h14-16,18-19,24-27,29-31,33-36H,13,17,20-23H2,1-12H3,(H,41,47)(H,42,48)(H,50,51)/t26-,27+,29-,30-,31+,33-,34-,35-,36+/m0/s1
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| Chemical Name |
((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(dimethylamino)-3-methylbutanamido)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoyl)-L-phenylalanine
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| Synonyms |
Auristatin F
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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: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 (~268.10 mM )
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (6.70 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 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 (6.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 50.0 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: ≥ 5 mg/mL (6.70 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 | 1.3405 mL | 6.7024 mL | 13.4048 mL | |
| 5 mM | 0.2681 mL | 1.3405 mL | 2.6810 mL | |
| 10 mM | 0.1340 mL | 0.6702 mL | 1.3405 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05755048 | Recruiting | Investigational drug: Recombinant Anti-HER2 Humanized Monoclonal Antibody Monomethyl Auristatin F Conjugates for Injection |
Breast Cancer | Shanghai Fosun Pharmaceutical Industrial Development Co | March 28, 2023 | Phase 3 |
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