Cat. No.: HY-145574

Iruplinalkib

(Synonyms: WX-0593)

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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.

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Pureté: 99.62%
CAS No.: 1854943-32-0
Formule: C₂₉H₃₈ClN₆O₂P
Masse moléculaire:569.08

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Iruplinalkib Chemical Structure

CAS No.: 1854943-32-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

ALK and ROS1^[1]

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform ERK :

Voir tous les produits spécifiques à Isoform STAT :

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]

In Vitro

Iruplinalkib (1.23-100 nM; 2 h) inhibits the growth of NCI-H3122 cells by inhibiting the phosphorylation of ALK, RAS/MAPK/ERK, PI3K/AKT^[1].
Iruplinalkib (10-1000 nM; 2 h) inhibits the phosphorylation of ROS1 and related pathway key proteins in NIH-3T3 (CD74-ROS1) and Ba/F3 (SLC34A2-ROS1) cells^[1].

MedChemExpress (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.

In Vivo

Iruplinalkib (2.5-10 mg/kg; Oral administration; 3 weeks) has antitumor effect in mouse model of non-small cell lung cancer^[1]

MedChemExpress (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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1854943-32-0
Appearance Solid
Masse moléculaire 569.08
Formule C₂₉H₃₈ClN₆O₂P
Color Off-white to light yellow
SMILES

O=P(C)(C)C1=C(NC2=NC(NC3=CC=C(N4CCC5(CCN(CC5)C)CC4)C=C3OC)=NC=C2Cl)C=CC=C1
Synonyms

WX-0593
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 10 mg/mL (17.57 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

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Iruplinalkib

Immunology/Inflammation Compound Library

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Lactylation Compound Library

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform ERK

Voir tous les produits spécifiques à Isoform STAT

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Iruplinalkib Related Classifications

HY-145574 Related Classifications