TASIN-1
Based on 1 Customer Validation
TASIN-1 is a selective inhibitor of truncated APCTR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer.
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- Pureza: 98.09%
- No. CAS: 792927-06-1
- Fòrmula: C18H28N2O3S
- Peso molecular:352.49
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Almacenamiento: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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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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Oxygen Sensing Compound Library
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Endoplasmic Reticulum Stress Compound Library
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Pyroptosis Compound Library
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Transcription Factor-Targeted Library
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Anti-Colorectal Cancer Compound Library
HY-L103
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Osteogenesis Compound Library
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Heterocyclic Compound Library
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Pain-Related Compound Library
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Highly Selective Activators Library
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Cell Death Library
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Multi-Target Compound Library
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Cell Proliferation Compound Library
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High-Throughput Bioactive Compound Library
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Lactylation Compound Library
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Apoptosis Compound Library
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Immunology/Inflammation Compound Library
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MAPK Compound Library
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Ver todos los productos específicos de isoformas Caspase
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Actividad biológica
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Caspase 3 |
Caspase-7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | IC50 |
63 nM
Compound: 6; TASIN-1
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Antiproliferative activity against human DLD1 cells after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human DLD1 cells after 72 hrs by Celltiter-Glo assay
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[PMID: 31070915] |
| HCT-116 | IC50 |
>5 μM
Compound: 6; TASIN-1
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Cytotoxicity against human HCT116 cells harboring wild-type APC after 72 hrs by Celltiter-Glo assay
Cytotoxicity against human HCT116 cells harboring wild-type APC after 72 hrs by Celltiter-Glo assay
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[PMID: 31070915] |
| HT-29 | IC50 |
53 nM
Compound: 6; TASIN-1
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Antiproliferative activity against human HT-29 cells after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human HT-29 cells after 72 hrs by Celltiter-Glo assay
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[PMID: 31070915] |
TASIN-1 selectively inhibits adenomatous polyposis coli truncated (APCTR) in DLD1 cells with IC50=70 nM[1].
TASIN-1 (70 nM; 72 h) significantly inhibits the proliferation of human colon cancer cells DLD1 (APCTR) with IC50 of 70 nM, and has a high selectivity against HCT116 (APCWT) cells with IC50 >50 μM[1].
TASIN-1 (2.5 μM; 7 d) inhibits soft agar colony formation of DLD1 cells, but has no significant effect on HCT116[1].
TASIN-1 (2.5 μM; 2-48 h) reduced the cholesterol synthesis rate and endogenous cholesterol levels in DLD1 cells, but had no effect on HCT116 cells[1].
TASIN-1 (2.5 μM; 24 h) induced the expression of endoplasmic reticulum stress marker CHOP and JNK phosphorylation, and activated caspase 3/7 activity in DLD1 cells, but no significant changes were observed in HCT116 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DLD1 (APCTR), HCT116 (APCWT)
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Concentration:0.01-100 μM
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Incubation Time:72 h
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Result:Showed an IC50 of 70 nM in DLD1 cells and >50 μM in HCT116 cells, demonstrating >700-fold selectivity for APCTR cells.
TASIN-1 (20, 40 mg/kg; ip; twice weekly; 90 or 100 days) reduces the number and size of colon polyps and inhibits tumor progression in the CPC;Apc mouse genetic colorectal cancer model without significant liver and kidney damage or weight loss[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice (5-6 weeks old, ~20 g) with DLD1/HT29 (APCTR) or HCT116 (APCWT) subcutaneous xenograft model[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal (i.p.) injection, twice daily (bid), 18 days
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Result:Reduced DLD1 and HT29 tumor volumes by 40%-60% compared to vehicle control, with increased cleaved caspase 3 and PARP in tumor lysates.
Showed no significant growth inhibition against HCT116 tumors.
Tumor histology revealed fragmented nuclei and increased apoptotic cells in treated groups.
Chemical Information
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No. CAS 792927-06-1
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Appearance Solid
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Peso molecular 352.49
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Fòrmula C18H28N2O3S
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Color White to off-white
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SMILES
CC1CCN(C2CCN(S(=O)(C3=CC=C(OC)C=C3)=O)CC2)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 25 mg/mL (70.92 mM; ultrasonic and warming and heat to 60°C; 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.09 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.
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 (287 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
[1]. Zhang L, et al. Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer. Sci Transl Med. 2016 Oct 19;8(361):361ra140. [Content Brief]
[2]. Zhang L, et al. Cholesterol Depletion by TASIN-1 Induces Apoptotic Cell Death through the ER Stress/ROS/JNK Signaling in Colon Cancer Cells. Mol Cancer Ther. 2018 May;17(5):943-951. [Content Brief]
[3]. Wang W, et al. Design and Synthesis of TASIN Analogues Specifically Targeting Colorectal Cancer Cell Lines with Mutant Adenomatous Polyposis Coli (APC). J Med Chem. 2019 May 23;62(10):5217-5241. [Content Brief]
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 | 2.8370 mL | 14.1848 mL | 28.3696 mL | 70.9240 mL |
| 5 mM | 0.5674 mL | 2.8370 mL | 5.6739 mL | 14.1848 mL | |
| 10 mM | 0.2837 mL | 1.4185 mL | 2.8370 mL | 7.0924 mL | |
| 15 mM | 0.1891 mL | 0.9457 mL | 1.8913 mL | 4.7283 mL | |
| 20 mM | 0.1418 mL | 0.7092 mL | 1.4185 mL | 3.5462 mL | |
| 25 mM | 0.1135 mL | 0.5674 mL | 1.1348 mL | 2.8370 mL | |
| 30 mM | 0.0946 mL | 0.4728 mL | 0.9457 mL | 2.3641 mL | |
| 40 mM | 0.0709 mL | 0.3546 mL | 0.7092 mL | 1.7731 mL | |
| 50 mM | 0.0567 mL | 0.2837 mL | 0.5674 mL | 1.4185 mL | |
| 60 mM | 0.0473 mL | 0.2364 mL | 0.4728 mL | 1.1821 mL |
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