Taltobulin (trifluoroacetate) manufacturers
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| | Taltobulin (trifluoroacetate) Basic information |
| | Taltobulin (trifluoroacetate) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : ≥ 39 mg/mL (66.36 mM) | | form | Solid | | color | White to off-white |
| | Taltobulin (trifluoroacetate) Usage And Synthesis |
| 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 |
| | Taltobulin (trifluoroacetate) Preparation Products And Raw materials |
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