Iruplinalkib (Synonyms: WX-0593)

目录号: HY-145574 纯度: 99.29%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Iruplinalkib (WX-0593) 是一种口服有效的和选择性的 ALK/ROS1 抑制剂。Iruplinalkib 能有效抑制 ALK 和突变型 ALK、EGFR 的酪氨酸自磷酸化，IC₅₀ 在 5.38 到 16.74 nM之间。Iruplinalkib 也是转运蛋白 MATE1、MATE2K、P-gp 和 BCRP 的强抑制剂。Iruplinalkib 可用于非小细胞肺癌的研究。

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Iruplinalkib Chemical Structure

CAS No. : 1854943-32-0

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生物活性
纯度 & 产品资料
参考文献

生物活性

Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC₅₀ between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer^[1]^[2].

IC₅₀ & Target

ALK and ROS1^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	1 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152P mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	11 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171T mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	12 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK T1151Tins mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	12 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring SLC34A2-ROS1-L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	13 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring ALK wild type assessed as reduction in cell viability by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	15 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986Y mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	17 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	21 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring ALK C1156Y mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	22 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174V mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	22 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-S1986F mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	24 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring ALK L1196M mutant assessed as reduction in cell viability by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	32 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK I1171S mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	33 nM Compound: 16a; WX-0593	Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against mouse BaF3 cells harbouring CD74-ROS1-D2033N mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	36 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK F1174C mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	4 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK L1152R mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
BaF3	IC₅₀	8 nM Compound: 16a; WX-0593	Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay Antiproliferative activity against crizotinib resistant mouse BaF3 cells expressing EML4 fused ALK V1180L mutant assessed as reduction in cell viability incubated for 72 hrs by Celltitre-Glo luminescent assay	[PMID: 35421578]
KARPAS-299	IC₅₀	14.5 nM Compound: 16a; WX-0593	Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay Antiproliferative activity against human KARPAS-299 cells harbouring wild type ALK assessed as reduction in cell viability by Celltitre-Glo luminescent assay	[PMID: 35421578]

体外研究
(In Vitro)

Iruplinalkib (1.23-100 nM；2 小时) 通过抑制 ALK、RAS/MAPK/ERK、PI3K/AKT 的磷酸化抑制 NCI-H3122 细胞的生长^[1]。
Iruplinalkib (10-1000 nM；2 小时) 在 NIH-3T3 (CD74-ROS1) 和 Ba/F3 (SLC34A2-ROS1) 细胞中抑制 ROS1 及相关通路关键蛋白的磷酸化^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

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

Western Blot Analysis^[1]

Cell Line:	NIH-3T3 (CD74-ROS1) and Ba/F3 (SLC34A2-ROS1) cells
Concentration:	10, 100 and 1000 nM
Incubation Time:	2 h
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
(In Vivo)

Iruplinalkib (2.5-10 mg/kg；口服；3 周) 在非小细胞肺癌小鼠模型中具有抗肿瘤的作用^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	EML4-ALK transfected NCI-H3122 treated female BALB/c nude mice (4-6 weeks old)^[1]
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.

Clinical Trial

分子量

569.08

Formula

C₂₉H₃₈ClN₆O₂P

CAS 号

1854943-32-0

性状

固体

颜色

Off-white to light yellow

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

细胞实验：

DMSO 中的溶解度 : 10 mg/mL (17.57 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

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μL

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计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.29%

选择批次：

Data Sheet (608 KB) SDS (252 KB)

COA (191 KB) HNMR (265 KB) LCMS (259 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Yang Y, et al. Iruplinalkib (WX 0593), a novel ALK/ROS1 inhibitor, overcomes crizotinib resistance in preclinical models for non-small cell lung cancer. Invest New Drugs. 2023 Apr;41(2):254-266. [Content Brief]

[2]. Shi Y, et al. Safety and activity of WX-0593 (Iruplinalkib) in patients with ALK- or ROS1-rearranged advanced non-small cell lung cancer: a phase 1 dose-escalation and dose-expansion trial. Signal Transduct Target Ther. 2022;7(1):25. [Content Brief]

Iruplinalkib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7572 mL	8.7861 mL	17.5722 mL	43.9306 mL
	5 mM	0.3514 mL	1.7572 mL	3.5144 mL	8.7861 mL
	10 mM	0.1757 mL	0.8786 mL	1.7572 mL	4.3931 mL
	15 mM	0.1171 mL	0.5857 mL	1.1715 mL	2.9287 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

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Iruplinalkib (Synonyms: WX-0593)

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