Taltobulin
Based on 3 publication(s) in Google Scholar
Taltobulin (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. Taltobulin inhibits the polymerization of purified tubulin, disrupts microtubule organization in cells, and induces mitotic arrest, as well as apoptosis.
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- Reinheit : 99.82%
- CAS. Nr.: 228266-40-8
- Formel: C27H43N3O4
- Molecular Weight:473.65
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Taltobulin
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Biologische Aktivität
Beschreibung
IC50 & Target
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Traditional Cytotoxic Agents |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| 1A9 | IC50 |
0.03 nM
Compound: HTI-286, SPA110
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Cytotoxicity against human 1A9 cells
Cytotoxicity against human 1A9 cells
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[PMID: 18314944] |
| 1A9 | IC50 |
0.3 nM
Compound: HTI286(SPA110)
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Antiproliferative activity against human 1A9 cells
Antiproliferative activity against human 1A9 cells
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[PMID: 18411048] |
| 1A9 | IC50 |
0.0002 μM
Compound: HTI-286, SPA 110
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Antiproliferative activity against human 1A9 cells after 4 days by SRB assay
Antiproliferative activity against human 1A9 cells after 4 days by SRB assay
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[PMID: 19102699] |
| 1A9 | IC50 |
0.2 nM
Compound: HTI-286, SPA 110
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Antiproliferative activity against human 1A9 cells after 4 days by SRB assay
Antiproliferative activity against human 1A9 cells after 4 days by SRB assay
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[PMID: 19102699] |
| HCT-15 | IC50 |
4.2 nM
Compound: 2
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Inhibitory concentration against HCT-15 cells was evaluated
Inhibitory concentration against HCT-15 cells was evaluated
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[PMID: 15341492] |
| KB | IC50 |
5 nM
Compound: HTI-286 (2)
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Compound was tested for the cytotoxicity against KB-8-5 cell line expressing P-glycoprotein; value ranges from 1.2-5 nM
Compound was tested for the cytotoxicity against KB-8-5 cell line expressing P-glycoprotein; value ranges from 1.2-5 nM
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[PMID: 15261296] |
| KB | IC50 |
2.3 nM
Compound: HTI-286 (2)
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Compound was tested for cytotoxicity against paclitaxel resistant KB-8-5 cell line expressing P-glycoprotein
Compound was tested for cytotoxicity against paclitaxel resistant KB-8-5 cell line expressing P-glycoprotein
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[PMID: 15261301] |
| KB | IC50 |
2.3 nM
Compound: 2
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Concentration required to inhibit tumor cell growth in KB-8-5 cells
Concentration required to inhibit tumor cell growth in KB-8-5 cells
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[PMID: 15341492] |
| KB | IC50 |
77.4 nM
Compound: 2
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Concentration required to inhibit tumor cell growth in KB-V1 cells
Concentration required to inhibit tumor cell growth in KB-V1 cells
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[PMID: 15341492] |
| KB | IC50 |
81 nM
Compound: 2
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Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure
Concentration required to kill human epidermoid KBV1 cell lines containing very high levels of P-glycoprotein after 3 days of continuous exposure
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[PMID: 15454219] |
| KB 3-1 | IC50 |
140 nM
Compound: HTI-286 (2)
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Compound was tested for the cytotoxicity against KB-V1 cell line expressing P-glycoprotein; value ranges from 40-140 nM
Compound was tested for the cytotoxicity against KB-V1 cell line expressing P-glycoprotein; value ranges from 40-140 nM
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[PMID: 15261296] |
| KB 3-1 | IC50 |
2 nM
Compound: HTI-286 (2)
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Compound was tested for the cytotoxicity against KB-3-1 cell line; value ranges from 0.6-2 nM
Compound was tested for the cytotoxicity against KB-3-1 cell line; value ranges from 0.6-2 nM
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[PMID: 15261296] |
| KB 3-1 | IC50 |
0.96 nM
Compound: HTI-286 (2)
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Compound was tested for cytotoxicity against paclitaxel sensitive KB-3-1 cell line
Compound was tested for cytotoxicity against paclitaxel sensitive KB-3-1 cell line
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[PMID: 15261301] |
| KB 3-1 | IC50 |
77 nM
Compound: HTI-286 (2)
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Compound was tested for cytotoxicity against paclitaxel resistant KB-V1 cell line expressing P-glycoprotein
Compound was tested for cytotoxicity against paclitaxel resistant KB-V1 cell line expressing P-glycoprotein
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[PMID: 15261301] |
| KB 3-1 | IC50 |
0.96 nM
Compound: 2
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Concentration required to inhibit tumor cell growth in KB-3-1 cells
Concentration required to inhibit tumor cell growth in KB-3-1 cells
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[PMID: 15341492] |
| KB 3-1 | IC50 |
1 nM
Compound: 2
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Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure
Concentration required to kill human epidermoid KB-3-1 cell lines containing very low levels of P-glycoprotein after 3 days of continuous exposure
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[PMID: 15454219] |
| KB 3-1 | IC50 |
2.4 nM
Compound: 2
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Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure
Concentration required to kill human epidermoid KB85 cell lines containing moderate levels of P-glycoprotein after 3 days of continuous exposure
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[PMID: 15454219] |
| LOX IMVI | IC50 |
1.4 nM
Compound: 2
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Inhibitory concentration against Lox melanoma cells
Inhibitory concentration against Lox melanoma cells
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[PMID: 15341492] |
| MCF7 | IC50 |
0.08 nM
Compound: 8, SPA110
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Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay
Cytotoxicity activity against human MCF7 cells expressing p53 mutant by MTT assay
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[PMID: 12608848] |
| MCF7 | IC50 |
0.09 nM
Compound: 8, SPA110
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Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay
Antimitotic activity against human MCF7 cells expressing p53 mutant by MTT assay
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[PMID: 12608848] |
| MCF7 | IC50 |
0.00015 μM
Compound: HTI-286, SPA 110
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Antiproliferative activity against human MCF7 cells after 4 days by SRB assay
Antiproliferative activity against human MCF7 cells after 4 days by SRB assay
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[PMID: 19102699] |
| MCF7 | IC50 |
0.15 nM
Compound: HTI-286, SPA 110
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Antiproliferative activity against human MCF7 cells after 4 days by SRB assay
Antiproliferative activity against human MCF7 cells after 4 days by SRB assay
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[PMID: 19102699] |
| NCI-H1299 | IC50 |
6.8 nM
Compound: 2
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Inhibitory concentration against NCI-H1299 cells was evaluated
Inhibitory concentration against NCI-H1299 cells was evaluated
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[PMID: 15341492] |
In Vitro
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. Further protocols information, click here.
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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).
In Vivo
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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CAS. Nr. 228266-40-8
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Appearance Solid
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Molecular Weight 473.65
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Formel C27H43N3O4
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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
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Synonyms
HTI-286; SPA-110
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 100 mg/mL (211.13 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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 (5.28 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 (5.28 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.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.06 mM); Clear solution
In Vivo Dissolution Calculator
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Reinheit & Dokumentation
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Data Sheet (301 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1113 mL | 10.5563 mL | 21.1126 mL | 52.7816 mL |
| 5 mM | 0.4223 mL | 2.1113 mL | 4.2225 mL | 10.5563 mL | |
| 10 mM | 0.2111 mL | 1.0556 mL | 2.1113 mL | 5.2782 mL | |
| 15 mM | 0.1408 mL | 0.7038 mL | 1.4075 mL | 3.5188 mL | |
| 20 mM | 0.1056 mL | 0.5278 mL | 1.0556 mL | 2.6391 mL | |
| 25 mM | 0.0845 mL | 0.4223 mL | 0.8445 mL | 2.1113 mL | |
| 30 mM | 0.0704 mL | 0.3519 mL | 0.7038 mL | 1.7594 mL | |
| 40 mM | 0.0528 mL | 0.2639 mL | 0.5278 mL | 1.3195 mL | |
| 50 mM | 0.0422 mL | 0.2111 mL | 0.4223 mL | 1.0556 mL | |
| 60 mM | 0.0352 mL | 0.1759 mL | 0.3519 mL | 0.8797 mL | |
| 80 mM | 0.0264 mL | 0.1320 mL | 0.2639 mL | 0.6598 mL | |
| 100 mM | 0.0211 mL | 0.1056 mL | 0.2111 mL | 0.5278 mL |
Taltobulin Related Classifications
HY-15584 Related Classifications
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