RET-IN-3
Based on 1 Customer Validation
RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC50 of 19 nM.
For research use only. We do not sell to patients.
- Purity: 99.51%
- CAS No.: 2414374-53-9
- Formula: C18H21N5O2
- Molecular Weight:339.39
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Liver Cancer Compound Library
HY-L101
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Biological Activity
IC50: 19 nM (RETV804M)[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.11 μM
Compound: 34
|
Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay
Inhibition of RET V804M mutant (unknown origin)expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay
|
[PMID: 32292556] |
| BaF3 | IC50 |
4 μM
Compound: 34
|
Inhibition of RET (unknown origin) expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay
Inhibition of RET (unknown origin) expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay
|
[PMID: 32292556] |
| BaF3 | IC50 |
9 μM
Compound: 34
|
Inhibition of KDR (unknown origin) expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay
Inhibition of KDR (unknown origin) expressed in human BaF3 cells assessed as reduction in cell viability incubated for 48 hrs by celltiter glo luminescence cell viability assay
|
[PMID: 32292556] |
RET-IN-3 exhibits 16 and 410 fold selectivity compared to wt-RET and KDR, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 2414374-53-9
-
Appearance Solid
-
Molecular Weight 339.39
-
Formula C18H21N5O2
-
Color Off-white to light yellow
-
SMILES
CN(C)CCCNC1=NC2=C(C3=CC(OCO4)=C4C=C3)C=NN2C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (294.65 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. 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. 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 (7.37 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.37 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 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Data Sheet (272 KB)
-
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)
- Portuguese - PT (393 KB)
-
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. 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 | 2.9465 mL | 14.7323 mL | 29.4646 mL | 73.6616 mL |
| 5 mM | 0.5893 mL | 2.9465 mL | 5.8929 mL | 14.7323 mL | |
| 10 mM | 0.2946 mL | 1.4732 mL | 2.9465 mL | 7.3662 mL | |
| 15 mM | 0.1964 mL | 0.9822 mL | 1.9643 mL | 4.9108 mL | |
| 20 mM | 0.1473 mL | 0.7366 mL | 1.4732 mL | 3.6831 mL | |
| 25 mM | 0.1179 mL | 0.5893 mL | 1.1786 mL | 2.9465 mL | |
| 30 mM | 0.0982 mL | 0.4911 mL | 0.9822 mL | 2.4554 mL | |
| 40 mM | 0.0737 mL | 0.3683 mL | 0.7366 mL | 1.8415 mL | |
| 50 mM | 0.0589 mL | 0.2946 mL | 0.5893 mL | 1.4732 mL | |
| 60 mM | 0.0491 mL | 0.2455 mL | 0.4911 mL | 1.2277 mL | |
| 80 mM | 0.0368 mL | 0.1842 mL | 0.3683 mL | 0.9208 mL | |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7366 mL |
Powered by Bioz