Taltobulin hydrochloride
Based on 3 publication(s) in Google Scholar
Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo. Taltobulin hydrochloride inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.34%
- Formula: C27H44ClN3O4
- Molecular Weight:510.11
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Taltobulin hydrochloride
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Biological Activity
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Traditional Cytotoxic Agents |
Taltobulin (HTI-286; 0.2-7.3 nM; 3 days) inhibits the growth of 18 tumor cell lines (leukemia, ovarian, NSCLC, breast, colon, and melanoma cell lines) with an average IC50 of 2.5±2.1 nM and a median value of 1.7 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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
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Concentration:0.2-7.3 nM
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Incubation Time:3 days
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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).
Taltobulin (HTI-286; 3 mg/kg; p.o. gavage) inhibits growth by 97.3 % and 82% in athymic nu/nu female mice with Lox melanoma xenografts and KB-3-1 epidermoid xenograft model, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic nu/nu female mice with Lox melanoma model (5-6 weeks of age)[1]
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Dosage:1.6 mg/kg
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Administration:Administered i.v.;for 35 days
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Result: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.
Chemical Information
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Appearance Solid
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Molecular Weight 510.11
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Formula C27H44ClN3O4
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Color White to off-white
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SMILES
CC(C)(C)[C@H](NC([C@H](C(C)(C1=CC=CC=C1)C)NC)=O)C(N([C@@H](C(C)C)/C=C(C(O)=O)\C)C)=O.Cl[H]
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Synonyms
HTI-286 hydrochloride; SPA-110 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Biomedicines
FGF1 Protects MCF-7 Cells against Taltobulin through Both the MEKs/ERKs and PI3K/AKT Signaling Pathway. [Abstract]2023 Jun 29;11(7):1856. PMID: 37509496 -
PLoS Negl Trop Dis
De novo identification of toxicants that cause irreparable damage to parasitic nematode intestinal cells. [Abstract]2020 May 26;14(5):e0007942. PMID: 32453724 -
Front Oncol
FGF1 protects FGFR1-overexpressing cancer cells against drugs targeting tubulin polymerization by activating AKT via two independent mechanisms. [Abstract]2022 Oct 6:12:1011762. PMID: 36276073
Solvent & Solubility
DMSO : ≥ 100 mg/mL (196.04 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 33.33 mg/mL (65.34 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.9604 mL | 9.8018 mL | 19.6036 mL | 49.0090 mL |
| 5 mM | 0.3921 mL | 1.9604 mL | 3.9207 mL | 9.8018 mL | |
| 10 mM | 0.1960 mL | 0.9802 mL | 1.9604 mL | 4.9009 mL | |
| 15 mM | 0.1307 mL | 0.6535 mL | 1.3069 mL | 3.2673 mL | |
| 20 mM | 0.0980 mL | 0.4901 mL | 0.9802 mL | 2.4505 mL | |
| 25 mM | 0.0784 mL | 0.3921 mL | 0.7841 mL | 1.9604 mL | |
| 30 mM | 0.0653 mL | 0.3267 mL | 0.6535 mL | 1.6336 mL | |
| 40 mM | 0.0490 mL | 0.2450 mL | 0.4901 mL | 1.2252 mL | |
| 50 mM | 0.0392 mL | 0.1960 mL | 0.3921 mL | 0.9802 mL | |
| 60 mM | 0.0327 mL | 0.1634 mL | 0.3267 mL | 0.8168 mL | |
| DMSO | 80 mM | 0.0245 mL | 0.1225 mL | 0.2450 mL | 0.6126 mL |
| 100 mM | 0.0196 mL | 0.0980 mL | 0.1960 mL | 0.4901 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Taltobulin hydrochloride Related Classifications
HY-15584B Related Classifications
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