1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. Soblidotin

Soblidotin  (Synonyms: Auristatin PE; TZT-1027)

Cat. No.: HY-14672 Purity: 99.64%
COA Handling Instructions

Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.

For research use only. We do not sell to patients.

Soblidotin Chemical Structure

Soblidotin Chemical Structure

CAS No. : 149606-27-9

Size Price Stock Quantity
1 mg USD 140 In-stock
5 mg USD 350 In-stock
10 mg USD 500 In-stock
25 mg USD 1000 In-stock
50 mg USD 1500 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Soblidotin

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Soblidotin (Auristatin PE) is a novel synthetic Dolastatin 10 derivative and inhibitor of tubulin polymerization.

IC50 & Target

Tubulin[1]

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

Intravenous injection of Auristatin PE (TZT-1027) has been shown to potently inhibit the growth of P388 leukemic cells and several solid tumors in mice, and to prolong the survival of the animals, and its antitumor efficacy has been shown to be superior or comparable to that of the reference agents Dolastatin 10, Cisplatin, Vincristine, and 5-Fluorouracil. Furthermore, in xenograft models, Auristatin PE reduces intratumoral blood perfusion 1 to >24 h after its administration, thereby producing hemorrhagic necrosis of the tumors[1]. Auristatin PE (Soblidotin) shows antivascular effects in tumoral models overexpressing VEGF and in murine colon tumors, with an increase in vascular permeability, vessel closure, and widespread hemorrhage[2]. Mice bearing subcutaneous HT-29 tumors (200 mm3) are dosed every 7 days with Auristatin PE (0.5 or 1.0 mg/kg) for a total of four cycles. Under such conditions, Auristatin PE (TZT-1027) inhibits the growth of HT-29 xenografts in a dose-dependent manner. Coadministration of Auristatin PE does not interfere with the PD184352-induced suppression of ERK1/2 phosphorylation. Immunostaining for Ki-67 as a marker for proliferating cells confirmed that the number of such cells in tumor sections is decreased greatly at 24 hours after the initial dosing with PD184352 compared with that apparent for vehicle-treated tumors. Auristatin PE treatment alone increases the number of TUNEL-positive cells in HT-29 xenografts by 24 hours in a dose-dependent manner, and this effect is enhanced by coadministration of PD184352[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

701.98

Formula

C39H67N5O6

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4245 mL 7.1227 mL 14.2454 mL
5 mM 0.2849 mL 1.4245 mL 2.8491 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.56 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.64%

References
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

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
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Soblidotin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Soblidotin
Cat. No.:
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