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ChemicalBook--->CAS DataBase List--->228266-41-9

228266-41-9

228266-41-9 Structure

228266-41-9 Structure
IdentificationBack Directory
[Name]

Taltobulin (trifluoroacetate)
[CAS]

228266-41-9
[Synonyms]

HTI-286 trifluoroacetate
SPA-110 trifluoroacetate
Taltobulin (trifluoroacetate)
HTI-286 TRIFLUOROACETATE;SPA-110 TRIFLUOROACETATE
[Molecular Formula]

C29H44F3N3O6
[MOL File]

228266-41-9.mol
[Molecular Weight]

587.671
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : ≥ 39 mg/mL (66.36 mM)
[form ]

Solid
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

Taltobulin trifluoroacetate (HTI-286 trifluoroacetate), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis[1].
[in vivo]

Taltobulin (HTI-286; 1.6 mg/kg i.v.) inhibits the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5) in athymic nu/nu female mice[1].
Taltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively[1].

Animal Model:Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)[1]
Dosage:1.6 mg/kg
Administration:Administered i.v.;for 35 days
Result:Growth of Lox tumors was inhibited by 96-98% on day 12 compared with vehicle-treated controls.
Growth of KB-8-5 tumors was inhibited by 84% on day 14 compared with vehicle-treated controls.
Growth of MX-1W tumors was inhibited by 97% compared with vehicle-treated controls.
Growth of DLD-1 and HCT-15 tumors was inhibited by 80 and 66%, respectively.
[IC 50]

Traditional Cytotoxic Agents
[References]

[1] Loganzo F, et al. HTI-286, a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Cancer Res. 2003 Apr 15;63(8):1838-45. PMID:12702571
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