1. Protein Tyrosine Kinase/RTK
    Apoptosis
    Autophagy
  2. ALK
    Apoptosis
    Autophagy
  3. ZX-29

ZX-29 

Cat. No.: HY-135887
Handling Instructions

ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.

For research use only. We do not sell to patients.

ZX-29 Chemical Structure

ZX-29 Chemical Structure

CAS No. : 2254805-62-2

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Description

ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect[1].

IC50 & Target

IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)[1]

In Vitro

ZX-29 (0-81 nM; 24-72 hours; NCI-H2228 cells) treatment leads to a time- and dose-dependent decrease in NCI-H2228 cell viability[1].
ZX-29 (10 nM; 24 hours; NCI-H2228 cells) treatment causes typical signs of autophagy and the formation of autophagosomes. ZX-29 enhances the expression level of LC3 and Beclin1[1].
ZX-29 (10 nM; 0-48 hours; NCI-H2228 cells) inhibits the proliferation of NCI-H2228 cells and arrests the cells in G1 phase[1].
ZX-29 (10-40 nM; 24-48 hours; NCI-H2228 cells) treatment induces apoptosis of NCI-H2228 cells. ZX-29 dose-dependently upregulates the expression levels of proapoptotic protein Bax, increases the production of activated forms of caspase 3, and downregulates the expression level of antiapoptotic protein Bcl-2[1].
ZX-29 (30-300 nM; 24 hours; NCI-H2228 cells) treatment significantly down-regulates the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner[1].
ZX-29 (20 nM; 0-48 hours; NCI-H2228 cells) treatment significantly increases the mRNA level of CHOP[1].
ZX-29 dose-dependently inhibits colony formation of NCI-H2228 cells. With an increase in ZX-29 concentration, the cell density decreased gradually, and the cells lost their normal morphology and become sharp and slender[1].

Cell Viability Assay[1]

Cell Line: NCI-H2228 cells
Concentration: 0 nM, 1 nM, 3 nM, 9 nM, 10 nM, 27 nM or 81 nM
Incubation Time: 24 hours, 48 hours or 72 hours
Result: Led to a time- and dose-dependent decrease in NCI-H2228 cell viability.

Cell Autophagy Assay[1]

Cell Line: NCI-H2228 cells
Concentration: 10 nM
Incubation Time: 24 hours
Result: Caused typical signs of autophagy and the formation of autophagosomes.

Cell Cycle Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 0 hour, 12 hours, 24 hours or 48 hours
Incubation Time: 24 hours
Result: Arrested the NCI-H2228 cells in G1 phase in a time-dependent manner.

Apoptosis Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 10 nM, 20 nM or 40 nM
Incubation Time: 24 hours, 48 hours
Result: Promoted NCI-H2228 cell apoptosis in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: NCI-H2228 cells
Concentration: 30 nM, 100 nM, 300 nM
Incubation Time: 24 hours
Result: Significantly down-regulated the expression of p-ALK and its downstream signaling proteins, including p-Akt and p-STAT3, in a dose-dependent manner.

RT-PCR[1]

Cell Line: NCI-H2228 cells
Concentration: 20 nM
Incubation Time: 0 hour, 6 hours, 12 hours, 24 hours or 48 hours
Result: The mRNA level of CHOP was increased significantly.
In Vivo

ZX-29 (50 mg/kg; intragastric administration; every 2 days; for a total of 7 times; female BALB/c nude mice) treatment suppresses tumor growth in a mouse xenograft model[1].

Animal Model: Female BALB/c nude mice (4-week-old) with H2228 cells[1]
Dosage: 50 mg/kg
Administration: Intragastric administration; every 2 days; for a total of 7 times
Result: Showed significantly attenuated tumor growth.
Molecular Weight

518.03

Formula

C₂₃H₂₈ClN₇O₃S

CAS No.

2254805-62-2

SMILES

CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

ZX-29ZX29ZX 29ALKApoptosisAutophagyAnaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Resistanceantitumorendoplasmicreticulump-Aktp-STAT3arrestBcl-2caspase-3CHOPERSInhibitorinhibitorinhibit

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