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

Auristatin PE (Synonyms: Soblidotin; TZT 1027; TZT-1027; TZT1027)

Cat. No.: HY-14672 Purity: 99.76%
Data Sheet SDS Handling Instructions

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

For research use only. We do not sell to patients.
Auristatin PE Chemical Structure

Auristatin PE Chemical Structure

CAS No. : 149606-27-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO $541 In-stock
1 mg $140 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
25 mg $1000 In-stock
50 mg $1500 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Description

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

IC50 & Target

Tubulin[1]

In Vitro

Auristatin PE (TZT-1027) is a novel synthetic dolastatin 10 derivative that inhibits tubulin polymerization. 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]. Auristatin PE (Soblidotin) is a synthetic analog of dolastatin 10 which inhibits the growth of several tumoral cell lines and induces caspase-3-dependent apoptosis. 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].

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00064220 Daiichi Sankyo Inc.|National Cancer Institute (NCI) Sarcoma April 2003 Phase 2
NCT00061854 Daiichi Sankyo Inc. Lung Cancer April 2003 Phase 2
NCT00072228 Daiichi Pharmaceuticals|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
10 mM 0.1425 mL 0.7123 mL 1.4245 mL
Animal Administration
[3]

Auristatin PE (TZT-1027) is dissolved in 0.05 Msodium lactate buffer (pH 4.5)[3].

Mice[3]
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
M.Wt

701.98

Formula

C₃₉H₆₇N₅O₆

CAS No.

149606-27-9

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO; Methanol: ≥ 44 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Auristatin PE
Cat. No.:
HY-14672
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