EML4-ALK kinase inhibitor 1
Based on 1 Customer Validation
EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 1373409-08-5
- Formula: C31H48N8O3
- Molecular Weight:580.76
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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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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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Biological Activity
IC50: 1 nM (EML4-ALK)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
1 nM
Compound: 12c
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Inhibition of EML4-fused ALK variant 1 (unknown origin) expressed in mouse BAF3 cells using peptide substrate measured after 1 hr by HTRF assay
Inhibition of EML4-fused ALK variant 1 (unknown origin) expressed in mouse BAF3 cells using peptide substrate measured after 1 hr by HTRF assay
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[PMID: 30878193] |
| BaF3 | IC50 |
9.7 nM
Compound: 12c
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Antiproliferative activity against mouse BAF3 cells expressing EML4-fused ALK variant 1 assessed as reduction in cell viability measured after 2 days by alamar blue assay
Antiproliferative activity against mouse BAF3 cells expressing EML4-fused ALK variant 1 assessed as reduction in cell viability measured after 2 days by alamar blue assay
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[PMID: 30878193] |
Chemical Information
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CAS No. 1373409-08-5
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Appearance Solid
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Molecular Weight 580.76
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Formula C31H48N8O3
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Color Light yellow to yellow
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SMILES
CO[C@H]1CC[C@H](NC2=C(CC)N=C(C(N)=O)C(NC3=CC(OC)=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)=N2)CC1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 110 mg/mL (189.41 mM; Need ultrasonic; 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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: ≥ 5.5 mg/mL (9.47 mM); Clear solution
This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 5.5 mg/mL (9.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (sealed storage, away from moisture and 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.
Purity & Documentation
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Data Sheet (271 KB)
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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)
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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, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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 | 1.7219 mL | 8.6094 mL | 17.2188 mL | 43.0470 mL |
| 5 mM | 0.3444 mL | 1.7219 mL | 3.4438 mL | 8.6094 mL | |
| 10 mM | 0.1722 mL | 0.8609 mL | 1.7219 mL | 4.3047 mL | |
| 15 mM | 0.1148 mL | 0.5740 mL | 1.1479 mL | 2.8698 mL | |
| 20 mM | 0.0861 mL | 0.4305 mL | 0.8609 mL | 2.1524 mL | |
| 25 mM | 0.0689 mL | 0.3444 mL | 0.6888 mL | 1.7219 mL | |
| 30 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4349 mL | |
| 40 mM | 0.0430 mL | 0.2152 mL | 0.4305 mL | 1.0762 mL | |
| 50 mM | 0.0344 mL | 0.1722 mL | 0.3444 mL | 0.8609 mL | |
| 60 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL | |
| 80 mM | 0.0215 mL | 0.1076 mL | 0.2152 mL | 0.5381 mL | |
| 100 mM | 0.0172 mL | 0.0861 mL | 0.1722 mL | 0.4305 mL |
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