Iruplinalkib (Synonyms:WX-0593)
目录号 : KM22287 CAS No. : 1854943-32-0 纯度 : 98%
Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.
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5mg
In-stock
10mg
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25mg
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50mg
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100mg 询价 In-stock
200mg 询价 In-stock
10 mM * 1 mL in DMSO
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生物活性
Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.
体外研究

Iruplinalkib (1.23-100 nM; 2 hours) inhibits the growth of NCI-H3122 cells by suppressing the phosphorylation of ALK, RAS/MAPK/ERK, and PI3K/AKT.
Iruplinalkib (10-1000 nM; 2 hours) inhibits phosphorylation of ROS1 and related pathway key proteins in NIH-3T3 (CD74-ROS1) and Ba/F3 (SLC34A2-ROS1) cells.

 

Western Blot Analysis

Cell Line: NCI-H3122 cells
Concentration: 1.23, 3.7, 11.1, 33.3 and 100 nM
Incubation Time: 2 hours
Result: Reduced the phosphorylation levels of ALK, AKT and ERK.

Western Blot Analysis

Cell Line: NIH-3T3 (CD74-ROS1) and Ba/F3 (SLC34A2-ROS1) cells
Concentration:
10, 100 and 1000 nM
Incubation Time: 2 hour
Result: Reduced the phosphorylation levels of ROS1 and AKT in NIH-3T3 cells.
Reduced the phosphorylation levels of ROS1, Erk and SHP-1 in Ba/F3 cells.
体内研究

Iruplinalkib (2.5-10 mg/kg; oral; 3 weeks) has anti-tumor effects in a mouse model of non-small cell lung cancer.

 

Animal Model: EML4-ALK transfected NCI-H3122 treated female BALB/c nude mice (4-6 weeks old)
Dosage: 2.5, 5 and 10 mg/kg
Administration: Oral administration (p.o.); 3 weeks
Result: Inhibited tumor growth.
Had inhibitory effects on the phosphorylation of ALK, AKT and ERK.
Decreased the levels of phosphorylation of STAT3 and STAT5.
Had no effect on the body weight.
 
 
分子式
C29H38ClN6O2P
分子量
569.08
CAS号
1854943-32-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO: 10 mg/mL (17.57 mM; ultrasonic and warming and heat to 60°C)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 1.7572 mL 8.7861 mL 17.5722 mL
5 mM 0.3514 mL 1.7572 mL 3.5144 mL
10 mM 0.1757 mL 0.8786 mL 1.7572 mL
*

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。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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