瑞他霉素盐酸盐 - CAS:857402-63-2 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	瑞他霉素盐酸盐
英文名称:	Retaspimycin Hydrochloride
别名:	瑞他霉素盐酸盐 IPI-504
CAS No:	857402-63-2	分子式:	C₃₁H₄₆ClN₃O₈	分子量:	624.17
CAS No:	857402-63-2
分子式:	C₃₁H₄₆ClN₃O₈
分子量:	624.17

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

R10267 瑞他霉素盐酸盐 ≥98% (psaitong)

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包装规格：

5mg in glass bottle

溶解性：

溶于DMSO（60mg/mL超声）

产品描述：

基本信息

产品编号：R10267
产品名称：Retaspimycin Hydrochloride
CAS:	857402-63-2	储存条件	粉末	-20℃	四年
分子式：	C31H46ClN3O8		溶于液体	-80℃	两年
分子量	624.17
化学名：	[(3R,5S,6R,7S,8E,10S,11S,12Z,14E)-6,20,22-trihydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16-oxo-21-(prop-2-enylamino)-17-azabicyclo[16.3.1]docosa-1(22),8,12,14,18,20-hexaen-10-yl] carbamate;hydrochloride
Solubility (25°C)	体外	DMSO	50mg/mL (80.11mM; Need ultrasonic)
		Ethanol
		Water
	体内	现配现用
＜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	1.6021mL	8.0106mL	16.0213mL
5mM	0.3204mL	1.6021mL	3.2043mL
10mM	0.1602mL	0.8011mL	1.6021mL

生物活性

产品描述

一种有效的 Hsp90 抑制剂，EC50 为119nM。

靶点/IC₅₀

HSP90

119nM (EC50)

GRP94

119nM (EC50)

体外研究

Retaspimycin (IPI-504) is a novel and highly soluble analog of 17AAG, an inhibitor of Hsp90. Retaspimycin can abrogate both the unfolded protein response element (UPRE) and ERSE-driven luciferase activity in non-treated U266 and MM.1s cells as well as in Tunicamycin (Tm)-treated cells. The IC50s for the inhibition of reporter gene activity by Retaspimycin are 196±56nM in U266 and 472±177nM in MM.1s for UPRE-luc activity and 213±140nM for the ERSE-driven activity in MM.1s cells.

Retaspimycin treatment leads to a dose-dependent decrease of p50ATF6 with EC50 of 237nM, consistent with the reportergene assay. The level of sXBP1 is decreased in the presence of Retaspimycin with an apparent EC50 between 300nM and 1μM. Incubation of Retaspimycin (IPI-504) potently suppresses both Akt and MAPKs phosphorylation in both sensitive and Trastuzumab-resistant cells. Total levels of Akt decreased in all 4 cell lines (BT474, SKBR-3, HCC1569, and HCC1569) in a dose-dependent manner. However, levels of total MAPKs are not significantly altered with Retaspimycin treatment.

体内研究

Retaspimycin (IPI-504) and Trastuzumab independently induce tumor regression of Trastuzumab-sensitive BT474 cellderived xenografts. Xenografts derived from BT474R cells continue to grow in the presence of Trastuzumab but are still sensitive to Retaspimycin. When used in combination, Retaspimycin and Trastuzumab add only marginal benefits to Retaspimycin monotherapy. Retaspimycin (100mg/kg) as a single agent is more efficacious than Trastuzumab in inhibiting tumor growth in HCC1569 xenografts. The combination is not significantly superior to Retaspimycin used as a single agent

推荐实验方法(仅供参考)

细胞实验：

Cell Assay

Hela cells are grown in Dulbecco’s modified Eagle’s medium containing 10% fetal bovine serum, 1ug/mL streptomycin and 1ug/mL penicillin. U266 and MM.1s are cultured in RPMI 1640 medium containing 15% fetal bovine serum, 1mM pyruvate, 1ug/mL streptomycin, and 1ug/mL penicillin. All the cell lines are maintained at 37°C in a humidified 5% CO2 atmosphere. Viability studies are performed using the vital mitochondrial function stain Alamar Blue. After cells are incubated in 96-well plates (200μL) ± Retaspimycin, 20μL of Alamar Blue is added and incubated for 4-6 h at 37°C. The Alamar Blue reduction is monitored using an Envision plate reader at λEM=544nm and λEM=590nm. The ratios obtained from drug-treated cells versus vehicle treated cells are quantified and plotted against drug concentration to give EC50 values. Caspase-3 and 7 activities are detected using the Caspase Glow kit.

动物实验:

Animal Administration

Mice

For all the experiments, 2×107 cells are injected into the right flanks of 10 mice for each experimental condition. Established tumors are treated with Trastuzumab, Retaspimycin, or the combination as following: Trastuzumab (10 mg/kg in sterile PBS) or sterile PBS (control) is given intraperitoneally twice weekly. Retaspimyci (100 mg/kg) is administered intraperitoneally thrice weekly. Retaspimyci, Trastuzumab, and the combination treatments are tolerable. No significant toxicity is noticed among the treatment arms. Tumor growth is measured with digital calipers as indicated and tumor volume is determined using the formula: (length×width2)×(π/6). At the end of the experiments, the animals are anesthetized with 1.5% isofluorane-air mixture and killed by cervical dislocation. Results are depicted as means of tumor volume±SE.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果