Soblidotin
Based on 1 publication(s) in Google Scholar
Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.
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- Pureté : 99.29%
- CAS No.: 149606-27-9
- Formule: C39H67N5O6
- Masse moléculaire:701.98
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Soblidotin
More
Activité biologique
Description
IC50 & Target
Tubulin[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Panel NCI-60 (60 carcinoma cell lines) | GI50 |
0.49 nM
Compound: 31; Soblidotin; TZT-1027
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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] |
In Vitro
Soblidotin (Auristatin PE) is a novel synthetic dolastatin 10 derivative that inhibits tubulin polymerization. Soblidotin (Auristatin PE) exhibits antitumor activity against p-glycoprotein-overexpressing cell lines established from colon cancer H116 and breast cancer-resistant protein-positive cell lines established from lung cancer PC-6, and is more potent than Vincristine, Paclitaxel, and Docetaxel against these cell lines[1]. Soblidotin (Auristatin PE) is a synthetic analog of dolastatin 10 which inhibits the growth of several tumoral cell lines and induces caspase-3-dependent apoptosis. Soblidotin (Auristatin PE) also shows antitumoral activity in Vincristine-, Docetaxel-, and Paclitaxel-resistant tumors, which makes it a potential chemotherapy drug for use in tumors which do not respond to other microtubule inhibitors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 149606-27-9
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Appearance Solid
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Masse moléculaire 701.98
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Formule C39H67N5O6
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Color White to off-white
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SMILES
O=C(N[C@@H](C(C)C)C(N([C@@H]([C@H](CC)C)[C@H](OC)CC(N1CCC[C@@]1([H])[C@H](OC)[C@@H](C)C(NCCC2=CC=CC=C2)=O)=O)C)=O)[C@H](C(C)C)N(C)C
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Synonyms
Auristatin PE; TZT-1027
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years * The compound is unstable in solutions, freshly prepared is recommended.
Publications (1)
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Journal Impact Factor
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Most Recent
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Mater Sci Eng C Mater Biol Appl
Targeted delivery of Auristatin PE to Hep G2 cells using folate - conjugated boron nitride nanotubes. [Abstract]2020 Apr:109:110509. PMID: 32228939
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (142.45 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (3.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Protocole
Animal Administration[3]
Mice[3]
Soblidotin (Auristatin PE) and Vinorelbine are dissolved in 0.05 M sodium lactate buffer (pH 4.5) and in PBS, respectively. Mice are treated every 7 d with PD184352 (200 mg/kg) or vehicle by oral administration (four times per day, every 6 h) and with Auristatin PE (0.25-2.5 mg/kg), Vinorelbine (5-20 mg/kg), or vehicle by i.v. injection (once per day, 1 h after the first PD184352 administration). Tumor volume is measured with digital calipers and calculated according to the following formula: (longest diameter)×(shortest diameter)2/2. Body weight, tumor volume, and toxicities are noted every 2 to 4 d for the duration of the experiment.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Yamamoto N, et al. Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative and inhibitor of tubulin polymerization, given weekly to advanced solid tumor patients for 3 weeks. Cancer Sci. 2009 Feb;100(2):316-21. [Content Brief]
[2]. Fanale D, et al. Stabilizing versus destabilizing the microtubules: a double-edge sword for an effective cancer treatment option? Anal Cell Pathol (Amst). 2015;2015:690916. [Content Brief]
[3]. Watanabe K, et al. Blockade of the extracellular signal-regulated kinase pathway enhances the therapeutic efficacy of microtubule-destabilizing agents in human tumor xenograft models. Clin Cancer Res. 2010 Feb 15;16(4):1170-8. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4245 mL | 7.1227 mL | 14.2454 mL | 35.6136 mL |
| 5 mM | 0.2849 mL | 1.4245 mL | 2.8491 mL | 7.1227 mL | |
| 10 mM | 0.1425 mL | 0.7123 mL | 1.4245 mL | 3.5614 mL | |
| 15 mM | 0.0950 mL | 0.4748 mL | 0.9497 mL | 2.3742 mL | |
| 20 mM | 0.0712 mL | 0.3561 mL | 0.7123 mL | 1.7807 mL | |
| 25 mM | 0.0570 mL | 0.2849 mL | 0.5698 mL | 1.4245 mL | |
| 30 mM | 0.0475 mL | 0.2374 mL | 0.4748 mL | 1.1871 mL | |
| 40 mM | 0.0356 mL | 0.1781 mL | 0.3561 mL | 0.8903 mL | |
| 50 mM | 0.0285 mL | 0.1425 mL | 0.2849 mL | 0.7123 mL | |
| 60 mM | 0.0237 mL | 0.1187 mL | 0.2374 mL | 0.5936 mL | |
| 80 mM | 0.0178 mL | 0.0890 mL | 0.1781 mL | 0.4452 mL | |
| 100 mM | 0.0142 mL | 0.0712 mL | 0.1425 mL | 0.3561 mL |
Soblidotin Related Classifications
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