TAI-1
Based on 1 Customer Validation
TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.60%
- No. CAS: 1334921-03-7
- Fòrmula: C24H21N3O3S
- Peso molecular:431.51
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Almacenamiento:Powder -20°C, 3 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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Kinase Inhibitor Library
HY-L009
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Anti-Cancer Compound Library
HY-L025
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Anti-Aging Compound Library
HY-L034
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Orally Active Compound Library
HY-L061
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Anti-Blood Cancer Compound Library
HY-L079
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Cell Death Library
HY-L162
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Anti-Hematopathy Compound Library
HY-L171
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Actividad biológica
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NEK2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
48.6 nM
Compound: 31
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Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay
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[PMID: 24773549] |
| HeLa | IC50 |
48.6 nM
Compound: 7
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Antiproliferative activity against human HeLa cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human HeLa cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
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[PMID: 32113126] |
| K562 | IC50 |
34.9 nM
Compound: 31
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Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay
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[PMID: 24773549] |
| K562 | IC50 |
34.9 nM
Compound: 7
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Antiproliferative activity against human K562 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human K562 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
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[PMID: 32113126] |
| MDA-MB-231 | IC50 |
32 nM
Compound: 31
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Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay
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[PMID: 24773549] |
| MDA-MB-231 | IC50 |
32 nM
Compound: 7
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Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
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[PMID: 32113126] |
| MDA-MB-468 | IC50 |
37 nM
Compound: 31
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Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay
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[PMID: 24773549] |
| MDA-MB-468 | IC50 |
37 nM
Compound: 7
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Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay
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[PMID: 32113126] |
TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death[1].
TAI-1 induces cancer cell death through the induction of cleavage of apoptotic proteins Caspase 3 and PARP and degradation of anti-apoptotic proteins MCL-1 and suggests that TAI-1 leads to activation of the apoptotic pathways[1].
TAI-1 is effective in many cancer cells, such as Chronic myeloid leukemia, Cervical cancer, Breast, metastatic-pleural, invasive ductal carcinoma, Acute myeloid leukemia, Myelogenous leukemia, Colorectal carcinoma cells, with GI50 less than 100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C.B-17 SCID mice (6-7 weeks, 21-24 g)[1].
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Dosage:20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.
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Administration:QDx28 cycles.
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Result:Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models.
Did not lead to any loss in body weight.
Chemical Information
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No. CAS 1334921-03-7
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Appearance Solid
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Peso molecular 431.51
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Fòrmula C24H21N3O3S
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Color White to off-white
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SMILES
O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(OC4=CC=C(OC)C=C4)C=C3C)=CS2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (231.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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.
Pureza y Documentación
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Ficha de datos (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 2.3174 mL | 11.5872 mL | 23.1744 mL | 57.9361 mL |
| 5 mM | 0.4635 mL | 2.3174 mL | 4.6349 mL | 11.5872 mL | |
| 10 mM | 0.2317 mL | 1.1587 mL | 2.3174 mL | 5.7936 mL | |
| 15 mM | 0.1545 mL | 0.7725 mL | 1.5450 mL | 3.8624 mL | |
| 20 mM | 0.1159 mL | 0.5794 mL | 1.1587 mL | 2.8968 mL | |
| 25 mM | 0.0927 mL | 0.4635 mL | 0.9270 mL | 2.3174 mL | |
| 30 mM | 0.0772 mL | 0.3862 mL | 0.7725 mL | 1.9312 mL | |
| 40 mM | 0.0579 mL | 0.2897 mL | 0.5794 mL | 1.4484 mL | |
| 50 mM | 0.0463 mL | 0.2317 mL | 0.4635 mL | 1.1587 mL | |
| 60 mM | 0.0386 mL | 0.1931 mL | 0.3862 mL | 0.9656 mL | |
| 80 mM | 0.0290 mL | 0.1448 mL | 0.2897 mL | 0.7242 mL | |
| 100 mM | 0.0232 mL | 0.1159 mL | 0.2317 mL | 0.5794 mL |
TAI-1 Related Classifications
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