| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Traditional Cytotoxic Agents
Tubulin (vinca site). Taltobulin hydrochloride binds to tubulin at the vinca alkaloid binding site, inhibiting tubulin polymerization and causing microtubule depolymerization. This leads to G2/M cell cycle arrest and subsequent apoptosis. It is a potent antimitotic agent with IC50 values in the low nanomolar range against various cancer cells. |
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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].
In vitro, Taltobulin hydrochloride potently inhibits the growth of a wide range of human cancer cell lines, including those with multidrug resistance (MDR) due to P-glycoprotein overexpression. It has IC50 values in the low nanomolar to low micromolar range. The compound induces G2/M arrest, disrupts the mitotic spindle, and activates caspase-dependent apoptosis. |
| 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].
Taltobulin hydrochloride has demonstrated significant antitumor activity in vivo in various murine xenograft models, including those resistant to paclitaxel and vincristine. In a human non-small cell lung cancer xenograft model, it produced tumor growth inhibition and regression. It is more potent than hemiasterlin and has a favorable toxicity profile in preclinical studies. |
| Enzyme Assay |
Tubulin polymerization assay: Purified tubulin (1 mg/mL) is incubated with increasing concentrations of Taltobulin hydrochloride (0-1000 nM) in polymerization buffer (80 mM PIPES, pH 6.9, 2 mM MgCl2, 0.5 mM EGTA, 1 mM GTP) at 37degC. Tubulin polymerization is monitored spectrophotometrically at 340 nm for 30-60 min. The IC50 for inhibition of polymerization is calculated by non-linear regression from the initial slope or final absorbance.
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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). Cell proliferation and apoptosis assay: Human cancer cells (e.g., HCT116, MDA-MB-231, or MDR variants) are seeded in 96-well plates (5,000 cells/well). Cells are treated with Taltobulin hydrochloride (0-1000 nM) for 48-72 h. Cell viability is measured by MTT or CellTiter-Glo. For cell cycle analysis, cells are treated for 24 h, fixed, stained with propidium iodide, and analyzed by flow cytometry. Apoptosis is assessed by Annexin V/PI staining or caspase-3/7 activity. |
| 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. Xenograft tumor model: Female athymic nude mice (6-8 weeks old) are subcutaneously implanted with human tumor cells (e.g., A549 lung cancer or HT-29 colon cancer, 5×10⁶ cells/mouse). When tumors reach ~100-200 mm3, mice are randomized into groups (n=6-10). Taltobulin hydrochloride is administered intravenously at doses of 0.5-5 mg/kg on a q4d×3 schedule or weekly. Tumor volume is measured twice weekly. Tumor growth inhibition (TGI) and regressions are recorded. |
| ADME/Pharmacokinetics |
Taltobulin hydrochloride is water-soluble and exhibits good pharmacokinetic properties. In preclinical species, it has a plasma half-life of 0.5-2 h, moderate clearance, and a volume of distribution consistent with tissue distribution. The compound is administered intravenously due to limited oral bioavailability. It shows dose-proportional exposure and good tumor penetration.
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| Toxicity/Toxicokinetics |
Toxicity data in preclinical studies: Taltobulin hydrochloride shows a tolerable safety profile with a therapeutic window. Dose-limiting toxicities in animals are consistent with antimitotic agents: myelosuppression (neutropenia, thrombocytopenia), gastrointestinal effects, and mild peripheral neuropathy at high doses. No significant organ toxicity was reported at effective doses. The compound is for research use only.
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| References | |
| Additional Infomation |
Taltobulin hydrochloride (HTI-286) is a research compound that has been evaluated in Phase I clinical trials for solid tumors, but development may not have progressed to approval. It is a potent vinca-site tubulin inhibitor that overcomes P-glycoprotein-mediated drug resistance. The CAS number for the free base is 194691-05-5. For research use only. Store at -20degC, protected from light and moisture.
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| Molecular Formula |
C27H44CLN3O4
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| Related CAS # |
Taltobulin;228266-40-8;Taltobulin trifluoroacetate;228266-41-9
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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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. |
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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