埃博霉素B - CAS:152044-54-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	埃博霉素B
英文名称:	Epothilone B
别名:	帕土匹龙 Patupilone;EPO906;1S,3S,7S,10R,11S,12S,16R)-7,11-dihydroxy-8,8,10,12,16-pentaethyl-3-((E)-1-(2-ethylthiazol-4-yl)prop-1-en-2-yl)-4,17-dioxabicyclo[14.1.0]heptadecane-5,9-dione
CAS No:	152044-54-7	分子式:	C₂₇H₄₁NO₆S	分子量:	507.68
CAS No:	152044-54-7
分子式:	C₂₇H₄₁NO₆S
分子量:	507.68

安全技术说明书(PDF) MSDS(PDF) 点击下载技术规格说明书(PDF) 点击下载产品说明书(PDF)

E10266 埃博霉素B ≥98% (psaitong)

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包装规格：

1mg 5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(≥100mg/mL )

产品描述：

基本信息

产品编号：E10266
产品名称：Epothilone B
CAS:	152044-54-7	储存条件	粉末	-20℃	四年
分子式：	C27H41NO6S		溶于液体	-80℃	六个月
分子量：	507.68			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	102mg/mL (200.91mM)
		Ethanol	102mg/mL (200.91mM)
		Water	Insoluble
	体内（现配现用）	30% PEG400+0.5% Tween80+5% propylene glycol	5mg/mL
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.9697mL	9.8487mL	19.6974mL
5mM	0.3939mL	1.9697mL	3.9395mL
10mM	0.1970mL	0.9849mL	1.9697mL
50mM	0.0394mL	0.1970mL	0.3939mL

生物活性

产品描述	一种微管稳定剂，i：0.71μ。
靶点/IC50	Tubulin (Cell-free assay)
靶点/IC50	1.8μM(EC0.01)
体外研究	Epothilone B inhibits HCT116 cells with IC50 of 0.8nM in HCT-116 cell line cytotoxicity assay.Epothilone B (Patupilone) is a microtubule (MT) targeting agent. As shown by MTT cell proliferation assay, after 72h of treatment Epothilone B efficiently inhibits cell growth with an IC50 of 6nM, while concentrations ≤1nM are not cytotoxic. Epothilone B significantly inhibits transwell cell migration at the non-cytotoxic concentration of 1nM, and the effect is more evident at 10nM.Epothilone B (Patupilone) is a novel, non-taxane-related and nonneurotoxic microtubule-stabilizing agent in human medulloblastoma cell lines. Epothilone B reduces the proliferative activity in the D341 cell line, with an IC50 of 0.53nM; in the D425Med cell line, with an IC50 of 0.37nM; and in the DAOY cell line, with an IC50 of 0.19nM. In the D341Med cell line,the effect of Epothilone B on clonogenic survival is at dose range of Epothilone B similar to the level of proliferative activity and viability (IC50, 0.50-0.75nM). However, the clonogenicity of D425Med and DAOY cells is already strongly reduced at a 10-fold lower concentration of Epothilone B (IC50, 30pM). These results overall demonstrate that Epothilone B is highly potent against different medulloblastoma cell lines.
体内研究	Treatment with Epothilone B (Patupilone) or ionizing radiation alone results in a partial tumor growth suppression over 10 days, whereas combined treatment exerts a strong supra-additive tumor growth control, with complete tumor regression in the follow-up period (P<0.005, for ionizing radiation or Epothilone B alone vs combined treatment).

推荐实验方法(仅供参考)

激酶实验：

Asp-Glu-Val-Asp (DEVD)ase activity is determined in cytosolic cell extracts. Cells are treated with increasing concentrations of Epothilone B (Patupilone) for 6, 12, 24, and 48h. Cells are harvested thereafter by trypsin/EDTA, centrifuged, and washed with precooled PBS. The cell pellet is suspended in 5 volumes of precooled buffer A (20mM HEPES-KOH [pH 7.5], 10mM KCl,1.5mM MgCl2, 1mM sodium EDTA, 1mM sodium EGTA, 1mM dithiothreitol [DDT], 250mM sucrose, and 0.1mM phenylmethylsulfonyl fluoride [PMSF] supplemented with protease inhibitors [5mg/mL pepstatin A, 10mg/mL leupeptin, 2mg/mL aprotinin, 2mg/mL DTT, and 1mM of PMSF]). After incubation on ice for 15 min, the cells are disrupted by freezing and thawing. Cell lysates are centrifuged at 1000g for 10 min at 4℃, and the supernatant is further centrifuged at 100 000g for 30 min. The resulting supernatant (S-100 fraction) is stored at −80℃. To determine caspase 3-like activity, 75μg of protein from the S-100 fraction is incubated at 37℃ with the colorimetric caspase 3 substrate N-acetyl-Asp-Glu-Val-Asp pnitroanilide (100mM; Ac-DEVD-pNA) and 1mM dATP in a final volume of 120μL. Cleavage of the caspase substrate is monitored at 405nm using a GenTec spectrophotometer.

细胞实验:

Human glioblastoma cells (U87MG, ATCC) are routinely maintained at 37℃and 5% CO2 in EMEM medium, with NEAA,containing 10% fetal bovine serum, 2mM of glutamine, 1% penicillin and streptomycin. U87MG cells are used for no more than 15 passages. Cells are seeded in 96-well plates (5000 cells/well). After 24h cells are treated with Epothilone B. Growth inhibition of U87MG cells is measured after 72h of drug treatment by using the MTT cell proliferation assay.

动物实验:

Mice

D425Med cells (6×106) are injected subcutaneously on the backs of 4-6-week-old athymic nude mice. Tumor volumes are determined from caliper measurements of tumor length (L) and width (l) according to the formula (L×l2)/2. Tumors are allowed to expand to a volume of 200mm3 (±10%) before treatment start. With the use of a customized shielding device,mice are given strictly loco regional radiotherapy of 3×3 Gy on 3 consecutive days using a Gulmay 200 kV X-ray unit at 100 cGy/min at room temperature. Epothilone B (2mg/kg; dissolved in 30% PEG-300/70% saline) is applied intravenously 24h before the first treatment with ionizing radiation (at day 0 of the treatment; n=5 per group). Tumor growth is monitored daily.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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