 Chemical Structure.png)
Physicochemical Properties
| Molecular Formula | C27H44CLN3O4 |
| Related CAS # | Taltobulin;228266-40-8;Taltobulin trifluoroacetate;228266-41-9 |
| Appearance | Typically exists as solid at room temperature |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | Traditional Cytotoxic Agents |
| ln Vitro | At a median IC50 of 1.7 nM and an average of 2.5±2.1 nM, taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines, including ovarian, breast, colon, melanoma, leukemia, and NSCLC cell lines[1]. |
| ln Vivo | In athymic nu/nu female mice, taltobulin (HTI-286; 1.6 mg/kg iv) suppresses the growth of human tumor xenografts (e.g., HCT-15, DLD-1, MX-1W, and KB-8-5)[1]. Taltobulin (HTI-286; 3 mg/kg; po gavage) suppresses growth in athymic nu/nu female mice using KB-3-1 epidermoid xenograft model and Lox melanoma xenograft model by 92.3% and 82.2%, respectively[1]. |
| Cell Assay |
Cell Proliferation Assay[1] Cell Types: Leukemia CCRF-CEM cell line; ovarian 1A9 cell line; NSCLC A549 and NCI-H1299 cell lines; breast MX-1W and MCF-7 cell lines; colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15 and Moser cell lines; melanoma A375, Lox and SK-Mel-2 cell lines Tested Concentrations: 0.2-7.3 nM Incubation Duration: 3 days Experimental Results: Inhibited the growth of tumor cell lines with IC50s of 0.2±0.03 nM(for leukemia CCRF-CEM cell line), 0.6±0.1 nM(for ovarian 1A9 cell line), 1.1±0.5 and 6.8±6.1 nM( for NSCLC A549 and NCI- H1299 cell lines), 1.8±0.6, 7.3±2.3 nM(for breast MX-1W, MCF-7 cell lines), 0.7±0.2, 1.1±0.4, 1.5±0.6, 1.8±0.6, 3.6±0.8, 3.7±2.0, 4.2±2.5, and 5.3±4.1 nM (for colon HCT-116, DLD-1, Colo205, KM20, SW620, S1, HCT-15, and Moser cell lines), 1.1±0.8, 1.4±0.6 and 1.7±0.5 nM (for melanoma A375, Lox and SK-Mel-2 cell lines). |
| Animal Protocol |
Animal/Disease Models: Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)[1] Doses: 1.6 mg/kg Route of Administration: Administered iv;for 35 days Experimental Results: 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. |
| References |
[1]. 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. |
Solubility Data
| Solubility (In Vitro) |
DMSO :≥ 100 mg/mL (~196.04 mM) H2O :~33.33 mg/mL (~65.34 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |