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Taltobulin (HTI-286) is a synthetic analog of the tripeptide cysteine, a microtubule protein inhibitor that inhibits liver tumor cell proliferation in vitro and tumor growth in vivo.Taltobulin is cytotoxic, induces mitotic arrest and apoptosis, and may be used in the study of breast cancer and microtubule tissue-related diseases.


| Description | Taltobulin (HTI-286) is a synthetic analog of the tripeptide cysteine, a microtubule protein inhibitor that inhibits liver tumor cell proliferation in vitro and tumor growth in vivo.Taltobulin is cytotoxic, induces mitotic arrest and apoptosis, and may be used in the study of breast cancer and microtubule tissue-related diseases. |
| In vitro | In leukemia CCRF-CEM cell line, ovarian 1A9 cell line, non-small cell lung cancer A549 cell line, and NCI-H1299 cell line, Taltobulin (0.2-7.3 nM; 3 days) inhibited the growth of tumor cell lines with IC50 values of 0.2±0.03 nM, 0.6±0.1 nM, 1.1±0.5 nM, and 6.8±6.1 nM, respectively[1]. |
| In vivo | In athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age), treatment with Taltobulin (1.6 mg/kg; administered i.v.; for 35 days) resulted in a 96-98% inhibition of Lox tumor growth on day 12 compared to the control group[1]. |
| Synonyms | SPA-110, HTI-286 |
| Molecular Weight | 473.65 |
| Formula | C27H43N3O4 |
| Cas No. | 228266-40-8 |
| Smiles | CN[C@H](C(=O)N[C@H](C(=O)N(C)[C@H](\C=C(/C)C(O)=O)C(C)C)C(C)(C)C)C(C)(C)c1ccccc1 |
| Relative Density. | 1.063 g/cm3 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (168.90 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.97 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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