RITA - CAS:213261-59-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	RITA
英文名称:	RITA
别名:	2,5-bis-(5-Hydroxymethyl-2-thienyl)-furan; NSC 652287
CAS No:	213261-59-7	分子式:	C₁₄H₁₂O₃S₂	分子量:	292.37
CAS No:	213261-59-7
分子式:	C₁₄H₁₂O₃S₂
分子量:	292.37
MDL:	MFCD03235294

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R10016 RITA ≥97%(HPLC) (psaitong)

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包装规格：

1mg 5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO( 58mgmg/ml)、乙醇、DMF PBS(PH7.2)。

产品描述：

基本信息

产品编号：R10016
产品名称：RITA
CAS:	213261-59-7	储存条件	粉末	-20℃	四年

分子式：	C14H12O3S2		溶于液体	-80℃	六个月
分子量	292.37			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	58mg/mL (198.37mM)
		Ethanol	8mg/mL (27.36mM)
		Water	Insoluble
	体内（现配现用）	30% propylene glycol, 5% Tween 80, 65% D5W	30mg/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	3.4203mL	17.1016mL	34.2032mL
5mM	0.6841mL	3.4203mL	6.8406mL
10mM	0.3420mL	1.7102mL	3.4203mL
50mM	0.0684mL	0.3420mL	0.6841mL

生物活性

产品描述	诱导DNA-蛋白质和DNA-DNA交联，检测不到DNA单链断裂，通过靶向作用于p53，也抑制MDM2-p53相互作用。
靶点/IC₅₀	Kd:1.5nM (p53dN) DNA Crosslinker
体外研究	RITA inhibits p53-HDM-2 interaction, binding to p53dN, with a Kd of 1.5nM. RITA (10μM) blocks complex formation between p53 and HDM-2 in HCT116 cells and HDFs and in NHF-ERMyc cells irrespective of c-Myc expression. RITA (0.5μM) reduces the viability of tumor cells in a wild-type p53-dependent manner. Moreover, RITA (0.1μM) induces p53-dependent apoptosis.RITA induces p53 but does not via DNA damage-signaling pathway. RITA (NSC 652287) induces DNA-DNA cross-links. RITA induces G2-M cell cycle arrest at 10 nM and causes apoptosis at 100nM. RITA (100nM) also elevates p53 and causes dosedependent effects on p21WAF1 protein levels. RITA inhibits the growth of HeLa and CaSki cells, with IC50s of 1 and 10μM. In addition,RITA (1μM) stabilizes p53 by inhibiting p53/E6AP interaction.
体内研究	RITA(0.1,1or10mg/kg,i.p.)shows potent antitumor activity in SCID mice bearing HCT116 and HCT116 TP53−/− xenografts. RITA (10mg/kg,i.p.) also suppresses the growth of HeLa cells in SCID mice.

推荐实验方法(仅供参考)

细胞实验:

For the cell viability assay, 3,000 cells per well are plated in a 96-well plate and treated with RITA for 48h, after which cell viability is assessed with the proliferation reagent WST-1. For colony formation assay, cells are seeded in 12-well plates and treated with RITA for 24h, after which the medium is replaced and the cells are allowed to grow for 10-14 d. The colonies are stained with crystal violet. For growth curves, 3000 cells/mL are plated in 12-well plates, treated with RITA,and counted over 5 d.

动物实验:

Mice

Female SCID mice, 4-6 weeks old, are implanted with subcutaneous xenografts using 1 × 106

cells in 90% Matrigel. Palpable tumors are established 3-6 d after the cells are injected, at which point RITA treatment is initiated. RITA is administered either 0.1, 1 or 10mg/kg every day by intravenous or intraperitoneal injection in a total volume of 100μL phosphate buffered saline.Xenografts are measured every 2 d. Tumor volumes are plotted for control and treated groups by dividing the average tumor volume for each data point by average starting tumor volume.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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