| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
TASIN-1 targets cells with truncated adenomatous polyposis coli (APC) mutations. The compound exerts its cytotoxic effects primarily by depleting cholesterol through inhibition of emopamil-binding protein (EBP) activity. TASIN-1 reduces endogenous cholesterol biosynthesis in APC-truncated cells but not in wild-type APC cells. The compound induces apoptotic cell death through the ER stress/ROS/JNK signaling pathway in colon cancer cells.
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| ln Vitro |
TASIN-1 exhibits potent and selective toxicity toward DLD1 cells (truncated APC) with an IC50 of 70 nM but shows no toxicity toward HCT116 cells (wild-type APC) with an IC50 >50 μM. TASIN-1 reduces endogenous cholesterol biosynthesis rate. The compound's cytotoxicity requires the presence of truncated APC; knockdown of truncated APC (>90%) expression desensitizes DLD1 cells to TASIN-1.
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| ln Vivo |
In nude mice with established DLD1 and HT29 tumors, intraperitoneal injection of TASIN-1 twice daily for 18 days reduced the size of tumor xenografts and tumor growth rates. TASIN-1 resulted in the appearance of apoptotic cells with fragmented nuclei and induced an increase in cleaved caspase 3 and cleaved PARP1. TASIN-1 did not inhibit tumor growth in HCT116 (wild-type APC) xenografts. In a genetically engineered CRC mouse model, TASIN-1 significantly reduced tumor formation in the colons.
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| Enzyme Assay |
Cellular assays for TASIN-1 employ colorectal cancer cell lines with APC mutations (e.g., DLD1, HT29) and APC-wild type cells (e.g., HCT116) as controls. Cells are treated with varying concentrations of TASIN-1 for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. IC50 values are calculated from concentration-response curves. Cholesterol biosynthesis is measured by monitoring incorporation of labeled precursors.
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| Cell Assay |
DLD1 cells (truncated APC) and HCT116 cells (wild-type APC) are seeded in multi-well plates and treated with varying concentrations of TASIN-1 for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining and by measuring cleaved caspase 3 and cleaved PARP1 by Western blot. Cholesterol levels are measured using enzymatic assays. ER stress and ROS levels are assessed by appropriate markers.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models using DLD1 and HT29 (APC-mutant) and HCT116 (wild-type APC) cells. Tumor-bearing mice are treated with TASIN-1 via intraperitoneal injection twice daily for 18 days. Tumor volumes are measured every 2-3 days. Apoptosis in tumor tissues is assessed by TUNEL staining and by measuring cleaved caspase 3 and cleaved PARP1. In a genetically engineered CRC mouse model, tumor formation in the colon is assessed.
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| ADME/Pharmacokinetics |
TASIN-1 has molecular formula C18H28N2O3S and molecular weight 352.49. It has CAS number 792927-06-1. The compound is soluble in DMSO (35.2 mg/mL), ethanol (12.02 mg/mL with ultrasonic), and water (2.45 mg/mL with gentle warming and ultrasonic). It should be stored as powder at -20°C for up to 3 years and in solvent at -80°C for up to 1 year.
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| Toxicity/Toxicokinetics |
Toxicological data for TASIN-1 are limited as it is a research compound. As a selective inhibitor targeting APC-mutant cells, it may have a favorable therapeutic index. The compound has been evaluated in preclinical models with acceptable tolerability. Standard safety pharmacology studies would be required for clinical development. The compound should be handled with appropriate laboratory safety precautions.
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| References | |
| Additional Infomation |
TASIN-1 is a selective inhibitor specifically targeting cancer cells harboring truncated adenomatous polyposis coli (APC) mutations, common in colorectal cancers. It selectively kills cells with APC truncations (IC50 = 70 nM) but spares cells with wild-type APC (IC50 > 50 μM). TASIN-1 reduces cholesterol biosynthesis and induces apoptosis through the ER stress/ROS/JNK signaling pathway. It is effective in vivo in mouse xenograft models.
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| Molecular Formula |
C18H28N2O3S
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|---|---|
| Molecular Weight |
352.491523742676
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| Exact Mass |
352.182
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| CAS # |
792927-06-1
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| Related CAS # |
1678515-13-3 (HCl);792927-06-1 (free);
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| PubChem CID |
1329829
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
480.0±55.0 °C at 760 mmHg
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| Flash Point |
244.1±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.557
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| LogP |
4.12
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
481
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1CCN(CC1)C2CCN(CC2)S(=O)(=O)C3=CC=C(C=C3)OC
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| InChi Key |
XCBHYDPDIJQQGM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H28N2O3S/c1-15-7-11-19(12-8-15)16-9-13-20(14-10-16)24(21,22)18-5-3-17(23-2)4-6-18/h3-6,15-16H,7-14H2,1-2H3
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| Chemical Name |
1-[1-(4-methoxyphenyl)sulfonylpiperidin-4-yl]-4-methylpiperidine
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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 |
| 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 : ~25 mg/mL (~70.92 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8370 mL | 14.1848 mL | 28.3696 mL | |
| 5 mM | 0.5674 mL | 2.8370 mL | 5.6739 mL | |
| 10 mM | 0.2837 mL | 1.4185 mL | 2.8370 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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