ARQ-092 - CAS:1313881-70-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	ARQ-092
英文名称:	ARQ-092
别名:	3-[3-[4-(1-氨基环丁基)苯基]-5-苯基-3H-咪唑并[4,5-b]吡啶-2-基]-2-吡啶胺 Miransertib;3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine
CAS No:	1313881-70-7	分子式:	C₂₇H₂₄N₆	分子量:	432.53
CAS No:	1313881-70-7
分子式:	C₂₇H₂₄N₆
分子量:	432.53

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

A10984 ARQ-092 ≥98% (psaitong)

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包装规格：

5mg 10mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO

产品描述：

基本信息

产品编号：	A10984
产品名称：	ARQ-092
CAS:	1313881-70-7	储存条件	粉末	-20℃	四年

分子式：	C27H24N6		溶于液体	-80℃	6个月
分子量：	432.53			-20℃	1个月
化学名：	Miransertib;3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine
Solubility (25°C)：
体外:	DMSO	8mg/mL (18.49mM)
	Ethanol	Insoluble
	Water	Insoluble
体内(现配现用):	请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照In Vitro⽅式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐是指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥1.25mg/mL(2.89mM);Clear solution
＜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	2.3120mL	11.5602mL	23.1203mL
5mM	0.4624mL	2.3120mL	4.6241mL
10mM	0.2312mL	1.1560mL	2.3120mL

生物活性

产品描述	一种有效的具有口服活性的选择性和变构Akt抑制剂。
靶点	Akt;Parasite
体外研究	In a large panel of cell lines derived from various tumor types,Miransertib (ARQ-092;Compound 21a) shows potent antiproliferative activity in cell lines containing PIK3CA/PIK3R1 mutations compared to those with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss.Miransertib shows excellent inhibition of p-Akt (S473) and p-Akt (T308) in both AN3CA and A2780 cells.The inhibition of the downstream protein p-PRAS40 (T246) is observed with Miransertib (IC50=0.31μM).Miransertib is markedly effective against intracellular amastigotes of L.donovani or L.amazonensis-infected macrophages.Miransertib also enhances mTOR dependent autophagy in Leishmania-infected macrophages MCE has not independently confirmed the accuracy of these methods.They are for reference only.
体内研究	Miransertib (ARQ-092;Compound 21a) shows good absolute oral bioavailability in rats (5mg/kg) and monkeys (10mg/kg) with F values of 62% and 49%,respectively.The half-life is longer in rats compared to monkeys with t1/2 values of 17h in rats versus 7h in monkeys.The Cmax is 198ng/mL and 258ng/mL and the AUCinf was 5496h•ng/mL and 2960h•ng/mL in rats and monkeys,respectively.Miransertib (ARQ-092;Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

推荐实验方法(仅供参考)

细胞实验:

Anti-proliferative cellular assays are conducted using the CellTiter Non-Radioactive Cell Proliferation Assay,which utilizes the production of formazan from a tetrazolium compound by live cells.AN3CA and A2780 cells are obtained from the ATCC.AN3CA cells are cultured in DMEM,and A2780 cells are cultured in RPMI.Cells are plated in 96-well plates at 2,000-10,000 cells/well,cultured for 24h,and treated with the test compound for 72h at a final DMSO concentration no greater than 0.5% v/v.PMS stock reagent (0.92mg/mL in DPBS) is diluted 20-fold in MTS stock reagent (2mg/mL in DPBS),and this MTS/PMS mixture is diluted 5-fold into each well of the 96-well plate.The plates are incubated for 3-4h,and the absorbance of formazan is measured at 490nm.The data are normalized to the untreated controls,the dose-response curves are fit to a four-parameter logistic equation,and the IC50 values are determined.All IC50 values reported are the geometric mean of at least two independent determinations.

动物实验:

Mice

SHP2Y279C/+ mice are used.Only male progeny are used for the experiments herein and all mice are maintained on outbred C57BL6/J backgrounds,backcrossed for more than 10 generations.Either vehicle or Miransertib (100mg/kg body weight) is then daily administered by oral gavage for 4 weeks.Administration began at 12 weeks of age (after established hypertrophy is indicated),and continued for 4 weeks,until the mice reach 16 weeks of age.As controls,SHP2+/+ and SHP2Y279C/+ mice are treated with vehicle alone.

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