硫链丝菌肽 | 1393-48-2

• 物质功能分类: 原料药 - 抗生素类药物 - 其它抗生素类药
• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 硫链丝菌肽
• 中文别名: 硫链丝菌素；硫链丝霉素
• 英文名称: N-[3-[(3-amino-3-oxoprop-1-en-2-yl)amino]-3-oxoprop-1-en-2-yl]-2-[(1R,11Z,15S,18S,25S,26R,35R,40S,46S,53S)-37-[(2S)-butan-2-yl]-18-[(2S,3R)-2,3-dihydroxybutan-2-yl]-11-ethylidene-59-hydroxy-8-[(1R)-1-hydroxyethyl]-31-[(1S)-1-hydroxyethyl]-26,40,46-trimethyl-43-methylidene-6,9,16,23,28,38,41,44,47-nonaoxo-27-oxa-3,13,20,56-tetrathia-7,10,17,24,36,39,42,45,48,52,58,61,62,63,64-pentadecazanonacyclo[23.23.9.329,35.12,5.112,15.119,22.154,57.01,53.032,60]tetrahexaconta-2(64),4,12(63),19(62),21,29(61),30,32(60),33,51,54,57-dodecaen-51-yl]-1,3-thiazole-4-carboxamide
• CAS: 1393-48-2
• 化学式: C₇₂H₈₅N₁₉O₁₈S₅
• 分子量: 1664.9
• InChiKey: NSFFHOGKXHRQEW-MRTIMCRRSA-N

物化性质

• 熔点：
  248-257°C (dec.)
• 比旋光度：
  D23 -98.5° (glacial acetic acid); -61° (dioxane); -20° (pyridine)
• 密度：
  1.0824 (rough estimate)
• 溶解度：
  溶于DMSO或氯仿

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S22,S24/25
• 危险类别码：
  R22
• WGK Germany：
  3
• 海关编码：
  29419090

制备方法与用途

生物活性

Thiostrepton 是一种抗生素，可选择性抑制 FOXM1。FOXM1 与 YAP/TEAD 复合物结合。YAP/TEAD/FOXM1 复合物在控制细胞周期的基因调控区域结合可能会影响细胞增殖。

体外研究

Thiostrepton (0.01-1000 μM; 48 hours) suppresses cell viability in A2780 and HEC-1A.

Cell Viability Assay

Cell Line:	A2780 and HEC-1A cells
Concentration:	0.01, 0.1, 1, 10, 100, 1000 μM
Incubation Time:	48 hours
Result:	The IC 50 s are 1.10 μM in A2780 and 2.22 μM in HEC-1A, respectively.

体内研究

Thiostrepton (i.p.; 17 mg/kg) reduces the tumorigenicity of Ewing's sarcoma (EWS) cells. Tumor volumes in control mice have increased ~6-fold from the initiation of treatment, while their Thiostrepton-treated counterparts increase only ~1.7-fold, exhibiting a ~3.5-fold reduction, relative to controls.

Animal Model:	Athymic (BALB/c nu/nu) nude mice bearing A4573 cells
Dosage:	17 mg/kg
Administration:	Administered i.p.
Result:	Treatment inhibited the growth of EWS-derived tumors in vivo.