中文名称: CAY10404
英文名称: CAY10404
CAS No: 340267-36-9
分子式: C17H12F3NO3S
分子量: 367.34
C10838 CAY10404 ≥98% (psaitong)
包装规格:
5mg 10mg in glass bottle
溶解性:
溶于DMSO(100 mg/mL 超声)
产品描述:

基本信息

产品编号:

C10838

产品名称:

CAY10404

CAS:

340267-36-9

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C17H12F3NO3S

溶于液体

-80℃

两年

分子量

367.34

-20℃

一个月

化学名: 

3-[4-(Methylsulfonyl)phenyl]-4-phenyl-5-(trifluoromethyl)-isoxazole

Solubility (25°C):

 

体外:

 

DMSO

100mg/mL(272.23mM;Need ultrasonic)

Ethanol

 

Water

 

体内(现配现用):

1.请依序添加每种溶剂:10% DMSO40% PEG3005% Tween-8045% saline,Solubility:2.5mg/mL(6.81mM);Suspended solution; Need ultrasonic

此⽅案可获得2.5mg/mL(6.81mM)的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到400μLPEG300中,混合均匀;向上述体系中加⼊50μLTween-80,混合均匀;然后继续加⼊450μL⽣理盐⽔定容⾄1mL。

2.请依序添加每种溶剂:10% DMSO90% (20% SBE-β-CD in saline)

Solubility:2.5mg/mL(6.81mM);Suspended solution; Need ultrasonic

此⽅案可获得2.5mg/mL(6.81mM)的均匀悬浊液,悬浊液可⽤于⼝服和腹腔注射。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中,混合均匀。

3.请依序添加每种溶剂:10% DMSO90% corn oil

Solubility:≥2.5mg/mL(6.81mM);Clear solution

此⽅案可获得≥2.5mg/mL(6.81mM,饱和度未知)的澄清溶液,此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例,取100μL25.0mg/mL的澄清DMSO储备液加到900μL⽟⽶油中,混合均匀。

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

2.7223mL

13.6114mL

27.2227mL

5mM

0.5445mL

2.7223mL

5.4445mL

10mM

0.2722mL

1.3611mL

2.7223mL

生物活性

产品描述

一种有效且高度选择性的环氧合酶2(COX-2)抑制剂,IC50为1nM,选择性指数(SI;COX-1IC50/COX-2IC50)为>500000。

靶点

COX-2

1nM(IC50)

COX-1

>500μM(IC50)

Akt

体外研究

CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC50>500µM)

CAY10404 (10-100µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC50) of 60-100µM

CAY10404 (20-100µM; for 3 days) induces apoptosis in NSCLC cells

CAY10404 (80µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β

CAY10404 (20, 50, 80, 100µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner

Cell Viability Assay

Cell Line:

Non-small cell lung cancer (NSCLC) cells (H1703, H358, H460)

Concentration:

10-100µM

Incubation Time:

For 3 days

Result:

Inhibited the growth of NSCLC cell lines in a concentration-dependent manner.

Apoptosis Analysis

Cell Line:

H460 cells

Concentration:

20, 50, 100µM

Incubation Time:

For 3 days

Result:

Induced apoptosis.

Western Blot Analysis

Cell Line:

NSCLC cells (H358, H460)

Concentration:

80µM

Incubation Time:

For 3 days

Result:

Induced a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-XL) and pAkt and pGSK-3β, without changing the level of the pro-apoptotic protein (Bax) and total Akt and GSK-3β protein levels.

体内研究

CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury

Animal Model:

Adult male C57Bl/6J mice weighing 24-30 g

Dosage:

50 mg/kg

Administration:

IP; daily; for 4 days

Result:

Attenuated cyclooxygenase activity, significantly decreasing BAL PGE2 and 6-keto PGF1α.
Decreased lung inflammation in HTV mice (high tidal volume; 20 ml/kg; for 4 hours) and attenuates ventilator-induced lung injury.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
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

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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

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  • 计算结果

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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