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描述 | CAY10566 is identified as a potent, orally bioavailable, and selective inhibitor of stearoyl-CoA desaturase1 (SCD1), exhibiting IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. It also demonstrates strong cellular efficacy in HepG2 cells by inhibiting the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs, with an IC50 of 7.9 nM or 6.8 nM[1].[2]. |
体内研究 | In vivo studies reveal that after the establishment of palpable tumors, treatment with CAY10566 at a dose of 2.5 mg/kg administered orally twice daily exhibits a more pronounced effect on Akt-driven tumors compared to Ras-driven tumors. The mean tumor volume, relative to untreated tumors by day 13 or 14 post-therapy, is significantly lower in the Akt-driven tumor group (0.5±0.04) than in the Ras-driven tumor group (0.67±0.05), with a P-value of 0.01 for the comparison between Ras and Akt-driven tumors as determined by a two-tailed t-test[4]. |
体外研究 | Additionally, CAY10566 concentration-dependently reduces the proliferation of Swiss 3T3 cells over 24 hours, with a concentration range of 0.0001-10 μM[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.57mL 0.51mL 0.26mL |
12.83mL 2.57mL 1.28mL |
25.65mL 5.13mL 2.57mL |
CAS号 | 944808-88-2 |
分子式 | C18H17ClFN5O2 |
分子量 | 389.811 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 25 mg/mL(64.13 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |