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TASIN-1 (Truncated APC Selective INhibitor-1) targets EBP- (Emopamil-binding protein; D8-D7 sterol isomerase) dependent cholesterol biosynthesis and selectively induces cellular cholesterol depletion and apoptotic death in human colorectal cancer (CRC) cultures harboring APC truncations under lipid-deficient conditions (0.2% FCS or 2% lipoprotein-deficient serum; IC50 from 35 nM/HT29 to 4.9 μM/HT55 in 72 hrs) as a result of defective cholesterol homeostasis regulation, while exhibiting little cytotoxicity toward wild-type APC CRC cells or non-transformed human colonic and bronchial epithelial cells (IC50 >50 μM in 72 hrs). TASIN-1 intraperitoneal injection is efficacious against the growth of CRC tumors with trunctated APC using the genetically engineered CPC;Apc mice (20 mg/kg twice a week) and two xenograft murine models (DLD1 & HT29; 40 mg/kg twice daily) without apparent toxicity to the animals.
| Molecular Weight | 388.95 |
| Formula | C18H28N2O3S · HCl |
| CAS Number | 1678515-13-3 |
| Solubility (25°C) | Water: 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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