ZX-29
Based on 1 Customer Validation
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.
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- Pureza: 98.59%
- No. CAS: 2254805-62-2
- Fòrmula: C23H28ClN7O3S
- Peso molecular:518.03
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Kinase Inhibitor Library
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Autophagy Compound Library
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Actividad biológica
IC50: 2.1 nM (ALK), 1.3 nM (ALK L1196M) and 3.9 nM (ALK G1202R)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H2228 cells
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Concentration:0 nM, 1 nM, 3 nM, 9 nM, 10 nM, 27 nM or 81 nM
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Incubation Time:24 hours, 48 hours or 72 hours
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Result:Led to a time- and dose-dependent decrease in NCI-H2228 cell viability.
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Cell Line:NCI-H2228 cells
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Concentration:10 nM
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Incubation Time:24 hours
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Result:Caused typical signs of autophagy and the formation of autophagosomes.
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Cell Line:NCI-H2228 cells
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Concentration:0 hour, 12 hours, 24 hours or 48 hours
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Incubation Time:24 hours
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Result:Arrested the NCI-H2228 cells in G1 phase in a time-dependent manner.
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Cell Line:NCI-H2228 cells
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Concentration:10 nM, 20 nM or 40 nM
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Incubation Time:24 hours, 48 hours
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Result:Promoted NCI-H2228 cell apoptosis in a dose-dependent manner.
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Cell Line:NCI-H2228 cells
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Concentration:30 nM, 100 nM, 300 nM
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Incubation Time:24 hours
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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.
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Cell Line:NCI-H2228 cells
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Concentration:20 nM
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Incubation Time:0 hour, 6 hours, 12 hours, 24 hours or 48 hours
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Result:The mRNA level of CHOP was increased significantly.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c nude mice (4-week-old) with H2228 cells[1]
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Dosage:50 mg/kg
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Administration:Intragastric administration; every 2 days; for a total of 7 times
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Result:Showed significantly attenuated tumor growth.
Chemical Information
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No. CAS 2254805-62-2
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Appearance Solid
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Peso molecular 518.03
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Fòrmula C23H28ClN7O3S
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Color Light yellow to green yellow
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SMILES
CS(=O)(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3OC)=NC=C2Cl)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 50 mg/mL (96.52 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)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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 (protect from light). 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 | 1.9304 mL | 9.6520 mL | 19.3039 mL | 48.2598 mL |
| 5 mM | 0.3861 mL | 1.9304 mL | 3.8608 mL | 9.6520 mL | |
| 10 mM | 0.1930 mL | 0.9652 mL | 1.9304 mL | 4.8260 mL | |
| 15 mM | 0.1287 mL | 0.6435 mL | 1.2869 mL | 3.2173 mL | |
| 20 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4130 mL | |
| 25 mM | 0.0772 mL | 0.3861 mL | 0.7722 mL | 1.9304 mL | |
| 30 mM | 0.0643 mL | 0.3217 mL | 0.6435 mL | 1.6087 mL | |
| 40 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
| 50 mM | 0.0386 mL | 0.1930 mL | 0.3861 mL | 0.9652 mL | |
| 60 mM | 0.0322 mL | 0.1609 mL | 0.3217 mL | 0.8043 mL | |
| 80 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.6032 mL |
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