| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Traditional Cytotoxic Agents
Tubulin. Taltobulin trifluoroacetate is a potent tubulin inhibitor that binds to tubulin and inhibits its polymerization. By disrupting microtubule dynamics, the compound induces mitotic arrest and apoptosis in cancer cells. It circumvents P-glycoprotein-mediated drug resistance. |
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| ln Vitro |
Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of eighteen tumor cell lines (melanoma, ovarian, breast, colon, NSCLC, and leukemia cell lines) with a median IC50 of 1.7 nM and an average of 2.5±2.1 nM[1].
Taltobulin trifluoroacetate inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest and apoptosis. HTI-286 significantly inhibits proliferation of hepatic tumor cell lines with a mean IC₅0 of 2 nM. The compound circumvents P-glycoprotein-mediated resistance. |
| ln 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 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]. In vivo, Taltobulin trifluoroacetate suppresses tumor growth, induces cell cycle arrest, and sensitizes cancer cells to other treatments. It circumvents P-glycoprotein-mediated resistance in vivo. Preclinical studies indicate it is a valuable therapeutic agent in oncology. |
| Enzyme Assay |
Microtubule polymerization assays are performed using purified tubulin. Tubulin is incubated with GTP and serial dilutions of test compound. Polymerization is monitored by turbidity at 340 nm over time. IC₅0 values for inhibition of polymerization are calculated from dose-response curves.
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| Cell Assay |
Cell Line: 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
Concentration: 0.2-7.3 nM Incubation Time: 3 days Result: 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). Cancer cell lines (e.g., hepatic tumor cell lines) are treated with Taltobulin trifluoroacetate at various concentrations. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell cycle analysis is performed by flow cytometry to assess mitotic arrest. Apoptosis is measured by caspase-3/7 activation or Annexin V staining. Microtubule organization is assessed by immunofluorescence. |
| Animal Protocol |
Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)[1]
1.6 mg/kg Administered i.v.;for 35 days Mice bearing subcutaneous tumor xenografts are administered Taltobulin trifluoroacetate via intravenous or intraperitoneal injection. Tumor growth is monitored by caliper measurements. Tumors are harvested for pharmacodynamic analysis of mitotic arrest, apoptosis markers, and microtubule disruption. Efficacy is determined by tumor growth inhibition. |
| ADME/Pharmacokinetics |
Taltobulin trifluoroacetate has a molecular weight of 587.67 g/mol and formula C2₉H44F3N3O₆. Standard PK parameters (half-life, Cmax, AUC, clearance, volume of distribution) would be determined in rodent studies. The compound is formulated in suitable vehicles for in vivo administration.
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| Toxicity/Toxicokinetics |
Toxicology data for Taltobulin trifluoroacetate are not publicly available. As a microtubule-targeting agent, potential toxicities may include neurotoxicity and myelosuppression, which are common to this class of agents. Standard preclinical safety assessment would include repeat-dose toxicology studies in rodents.
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| References | |
| Additional Infomation |
Taltobulin trifluoroacetate is a research compound for oncology studies. It is not clinically approved. The compound is a synthetic analogue of the tripeptide hemiasterlin and a potent antimicrotubule agent. It circumvents P-glycoprotein-mediated resistance, making it useful for studying drug resistance mechanisms and developing novel anticancer therapies.
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| Molecular Formula |
C₂₉H₄₄F₃N₃O₆
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|---|---|
| Molecular Weight |
587.67
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| Exact Mass |
587.318
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| CAS # |
228266-41-9
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| Related CAS # |
Taltobulin;228266-40-8;Taltobulin hydrochloride
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| PubChem CID |
92044389
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| Appearance |
White to off-white solid
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
41
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| Complexity |
829
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| Defined Atom Stereocenter Count |
3
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| SMILES |
FC(C(=O)O[H])(F)F.O=C([C@]([H])(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])N([H])C([C@]([H])(C(C([H])([H])[H])(C([H])([H])[H])C1C([H])=C([H])C([H])=C([H])C=1[H])N([H])C([H])([H])[H])=O)N(C([H])([H])[H])[C@]([H])(/C(/[H])=C(/C(=O)O[H])\C([H])([H])[H])C([H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
SHWPCKJNFBDPFA-LPWSJWOVSA-N
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| InChi Code |
InChI=1S/C27H43N3O4.C2HF3O2/c1-17(2)20(16-18(3)25(33)34)30(10)24(32)22(26(4,5)6)29-23(31)21(28-9)27(7,8)19-14-12-11-13-15-19;3-2(4,5)1(6)7/h11-17,20-22,28H,1-10H3,(H,29,31)(H,33,34);(H,6,7)/b18-16+;/t20-,21-,22-;/m1./s1
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| Chemical Name |
(E,4S)-4-[[(2S)-3,3-dimethyl-2-[[(2S)-3-methyl-2-(methylamino)-3-phenylbutanoyl]amino]butanoyl]-methylamino]-2,5-dimethylhex-2-enoic acid;2,2,2-trifluoroacetic acid
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| Synonyms |
HTI-286 trifluoroacetate; HTI-286; HTI286; SPA-110; SPA110; Taltobulin trifluoroacetate; SPA-110 trifluoroacetate
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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: ≥ 39 mg/mL (~66.4 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7016 mL | 8.5082 mL | 17.0164 mL | |
| 5 mM | 0.3403 mL | 1.7016 mL | 3.4033 mL | |
| 10 mM | 0.1702 mL | 0.8508 mL | 1.7016 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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