SML1988

TASIN-1 hydrochloride

≥98% (HPLC)

• Synonyme(s) : 1′-(4-Methoxyphenylsulfonyl)-4-methyl-1,4′-bipiperidine hydrochloride, 1,4′-Bipiperidine, 1′-[(4-methoxyphenyl)sulfonyl]-4-methyl-, hydrochloride, Truncated APC Selective INhibitor-1
• Formule empirique (notation de Hill) : C₁₈H₂₈N₂O₃S · HCl
• Numéro CAS: 1678515-13-3
• Poids moléculaire : 388.95
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Essai: ≥98% (HPLC)
• Forme: powder
• Conditions de stockage: desiccated; protect from light
• Couleur: white to beige
• Solubilité: H₂O: 2 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: CC(CC1)CCN1C(CC2)CCN2S(C3=CC=C(OC)C=C3)(=O)=O.[H]Cl
• Clé InChI: TXDTUQPRRXNCLP-UHFFFAOYSA-N

Description

Actions biochimiques/physiologiques

EBP-dependent cholesterol synthesis inhibitor with selective cytotoxicity against colorectal cancer cells harboring APC truncations.

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.

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable