Auristatin F
Based on 1 Customer Validation
Auristatin F is a potent cytotoxin in antibo-conjugated agents and an analogue of MMAF. Auristatin F is a potent microtubule inhibitor and vascular damaging agent (VDA). Auristatin F inhibits cell division by preventing tubulin aggregation.Auristatin F can be used in antibody-drug conjugates (ADC) .
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- Reinheit: 99.96%
- CAS. Nr.: 163768-50-1
- Formel: C40H67N5O8
- Molecular Weight:745.99
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years
* The compound is unstable in solutions, freshly prepared is recommended.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Microtubule[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Panel NCI-60 (60 carcinoma cell lines) | IC50 |
105 nM
Compound: 37
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Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition
Cytotoxicity against human Panel NCI-60 (60 carcinoma cell lines) assessed as cell growth inhibition
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[PMID: 35072477] |
Auristatin F and Monomethyl Auristatin F (MMAF) are potent ADC cytotoxin used in antibody-drug conjugates[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[2]
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Dosage:5 mg/kg
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Administration:Intravenous injection
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Result:
1.19 Parameter Dose (i.v.) mg/kg 5 Cmax (ng/mL) 8276.76 AUClast (min*ng/mL) 62661.30 CL (mL/min/ng) 77.33 Vss (mL/Kg) 1057.13
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 163768-50-1
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Appearance Solid
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Molecular Weight 745.99
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Formel C40H67N5O8
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Color White to light yellow
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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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Lösungsmittel & Löslichkeit
DMSO : 200 mg/mL (268.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (6.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (6.70 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * The compound is unstable in solutions, freshly prepared is recommended.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Roy S, et al. SMI-Ribosome inactivating protein conjugates selectively inhibit tumor cell growth. Chem Commun (Camb). 2017 Apr 11;53(30):4234-4237. [Content Brief]
[2]. Park MH, et, al. Pharmacokinetic and Metabolism Studies of Monomethyl Auristatin F via Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry. Molecules. 2019 Jul 29;24(15):2754. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.3405 mL | 6.7025 mL | 13.4050 mL | 33.5125 mL |
| 5 mM | 0.2681 mL | 1.3405 mL | 2.6810 mL | 6.7025 mL | |
| 10 mM | 0.1341 mL | 0.6703 mL | 1.3405 mL | 3.3513 mL | |
| 15 mM | 0.0894 mL | 0.4468 mL | 0.8937 mL | 2.2342 mL | |
| 20 mM | 0.0670 mL | 0.3351 mL | 0.6703 mL | 1.6756 mL | |
| 25 mM | 0.0536 mL | 0.2681 mL | 0.5362 mL | 1.3405 mL | |
| 30 mM | 0.0447 mL | 0.2234 mL | 0.4468 mL | 1.1171 mL | |
| 40 mM | 0.0335 mL | 0.1676 mL | 0.3351 mL | 0.8378 mL | |
| 50 mM | 0.0268 mL | 0.1341 mL | 0.2681 mL | 0.6703 mL | |
| 60 mM | 0.0223 mL | 0.1117 mL | 0.2234 mL | 0.5585 mL | |
| 80 mM | 0.0168 mL | 0.0838 mL | 0.1676 mL | 0.4189 mL | |
| 100 mM | 0.0134 mL | 0.0670 mL | 0.1341 mL | 0.3351 mL |
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