Soblidotin, Inhibitor

Soblidotin

Cat. Num. AAA5754546

• Purity: 98.00%
• Synonyms: Soblidotin; Auristatin PE; TZT-1027; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 100mg/mL (142.45mM) Need ultrasonic; H2O: <0.1mg/mL (insoluble); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C39H67N5O6
• 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
• CAS Number: 149606-27-9
• Target & IC50: Tubulin
• In Vitro: 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]. 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. Coadministration of Auristatin PE does not interfere with the PD184352-induced suppression of ERK1/2 phosphorylation. Furthermore, in xenograft models, Auristatin PE reduces intratumoral blood perfusion 1 to >24 hours after its administration, thereby producing hemorrhagic necrosis of the tumors[1]. Mice bearing subcutaneous HT-29 tumors (200mM3) are dosed every 7 days with Auristatin PE (0.5 or 1.0mg/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. 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].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Soblidotin, inhibitor

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

Product Categories/Family for Soblidotin, inhibitor

Cytoskeletal Signaling; Microtubule Associated

References

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.
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.
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.
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.
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.
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.