CH7057288
Based on 1 Customer Validation
CH7057288 is a potent and selective TRK inhibitor. CH7057288 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 2095616-82-1
- Formula: C32H31N3O5S
- Molecular Weight:569.67
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Kinase Inhibitor Library
HY-L009
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Neuronal Signaling Compound Library
HY-L013
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Protein Tyrosine Kinase Compound Library
HY-L016
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Anti-Cancer Compound Library
HY-L025
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Heterocyclic Compound Library
HY-L138
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Brain Cancer Compound Library
HY-L188
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Protein Kinase Compound Library
HY-L196
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
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Alkyne Compound Library
HY-L258
Biological Activity
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TRK |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NIH3T3 | IC50 |
8.4 nM
Compound: 7; CH7057288
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Antiproliferative activity against human NIH3T3 cells expressing MPRIP-NTRK1 assessed as cell growth inhibition incubated for 4 to 7 days by CellTiter-Glo Luminescent Cell Viability Assay
Antiproliferative activity against human NIH3T3 cells expressing MPRIP-NTRK1 assessed as cell growth inhibition incubated for 4 to 7 days by CellTiter-Glo Luminescent Cell Viability Assay
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[PMID: 36066182] |
CH7057288 induces regression of intracranial tumors and greatly improves event-free survival in an intracranial implantation model mimicking brain metastasis. CH7057288 can be a promising therapeutic agent for TRK fusion-positive cancer. TRK receptor tyrosine kinases are expressed as fusion proteins encoded by various fusion genes across a wide variety of cancer types, including lung and colorectal cancer[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2095616-82-1
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Appearance Solid
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Molecular Weight 569.67
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Formula C32H31N3O5S
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Color Off-white to yellow
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SMILES
O=C1C2=C(OC3=CC(C#CC4=CC(C(NC(C)(C)C)=O)=CC(C)=N4)=CC=C23)C(C)(C)C5=CC(NS(C)(=O)=O)=CC=C15
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 34 mg/mL (59.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.75 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
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.
Purity & Documentation
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Data Sheet (269 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7554 mL | 8.7770 mL | 17.5540 mL | 43.8851 mL |
| 5 mM | 0.3511 mL | 1.7554 mL | 3.5108 mL | 8.7770 mL | |
| 10 mM | 0.1755 mL | 0.8777 mL | 1.7554 mL | 4.3885 mL | |
| 15 mM | 0.1170 mL | 0.5851 mL | 1.1703 mL | 2.9257 mL | |
| 20 mM | 0.0878 mL | 0.4389 mL | 0.8777 mL | 2.1943 mL | |
| 25 mM | 0.0702 mL | 0.3511 mL | 0.7022 mL | 1.7554 mL | |
| 30 mM | 0.0585 mL | 0.2926 mL | 0.5851 mL | 1.4628 mL | |
| 40 mM | 0.0439 mL | 0.2194 mL | 0.4389 mL | 1.0971 mL | |
| 50 mM | 0.0351 mL | 0.1755 mL | 0.3511 mL | 0.8777 mL |
CH7057288 Related Classifications
HY-107362 Related Classifications
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