| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Traditional Cytotoxic Agents
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| 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].
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| 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].
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| 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]. 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.
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| Molecular Formula |
C27H44CLN3O4
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|---|---|
| Molecular Weight |
510.11
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| Related CAS # |
Taltobulin;228266-40-8;Taltobulin trifluoroacetate;228266-41-9
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| 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)
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| Solubility (In Vitro) |
DMSO :≥ 100 mg/mL (~196.04 mM)
H2O :~33.33 mg/mL (~65.34 mM) |
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| 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. View More
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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9604 mL | 9.8018 mL | 19.6036 mL | |
| 5 mM | 0.3921 mL | 1.9604 mL | 3.9207 mL | |
| 10 mM | 0.1960 mL | 0.9802 mL | 1.9604 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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