Enrupatinib
Based on 1 Customer Validation
Enrupatinib (EI‐1071) is a potent, orally active, CNS-penetrant and selective CSF1R inhibitor. Enrupatinib inhibits macrophage proliferation and osteoclast differentiation in vitro. Enrupatinib preserves microglia distal to Aβ plaques. Enrupatinib mitigates Alzheimer's disease (AD)-related pathologies by reducing neuroinflammation, preserving neuronal integrity, lowering disease-associated microglia gene expression, and enhancing cognitive function in 5xFAD and J20 mouse models. Enrupatinib reduces tumor-associated macrophage infiltration and enhances antitumor activity of anti-PD-1 antibody in murine colorectal cancer and breast cancer models. Enrupatinib can be used for the research of AD, colorectal cancer, and breast cancer.
For research use only. We do not sell to patients.
- Purity: 98.90%
- CAS No.: 2222689-47-4
- Formula: C27H26N6O3
- Molecular Weight:482.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Clinical Compound Library
HY-L026
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CNS-Penetrant Compound Library
HY-L028
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Drug Repurposing Compound Library
HY-L035
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Orally Active Compound Library
HY-L061
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Blood Cancer Compound Library
HY-L079
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Neurodegenerative Disease-related Compound Library
HY-L086
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Anti-Colorectal Cancer Compound Library
HY-L103
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Membrane Protein-targeted Compound Library
HY-L149
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Highly Selective Inhibitors Library
HY-L158
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Cytokine Inhibitors Library
HY-L161
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Anti-Hematopathy Compound Library
HY-L171
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Macrophage Related Compound Library
HY-L174
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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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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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
HY-L205
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Posttranslational Modification Library
HY-L226
Biological Activity
Enrupatinib inhibits CSF-1R activity in human monocytes/macrophages, AML-5 leukemia cells, MNFS-60 leukemia cells, and human osteoclasts[2].
Enrupatinib shows favorable ADME properties, including hepatocyte stability, high Caco-2 permeability, and favorable pharmacokinetic profiles[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2222689-47-4
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Appearance Solid
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Molecular Weight 482.53
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Formula C27H26N6O3
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Color Light yellow to green yellow
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SMILES
N#CC1=C2N=C(N3CCOCC3)C=NC2=CC=C1NC4=CC=C(C(OC)=C4)OCC5=CN=C(C)C=C5
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Synonyms
EI‐1071
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (207.24 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. 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 (5.18 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.
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 (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, 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 |
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| DMSO | 1 mM | 2.0724 mL | 10.3621 mL | 20.7241 mL | 51.8103 mL |
| 5 mM | 0.4145 mL | 2.0724 mL | 4.1448 mL | 10.3621 mL | |
| 10 mM | 0.2072 mL | 1.0362 mL | 2.0724 mL | 5.1810 mL | |
| 15 mM | 0.1382 mL | 0.6908 mL | 1.3816 mL | 3.4540 mL | |
| 20 mM | 0.1036 mL | 0.5181 mL | 1.0362 mL | 2.5905 mL | |
| 25 mM | 0.0829 mL | 0.4145 mL | 0.8290 mL | 2.0724 mL | |
| 30 mM | 0.0691 mL | 0.3454 mL | 0.6908 mL | 1.7270 mL | |
| 40 mM | 0.0518 mL | 0.2591 mL | 0.5181 mL | 1.2953 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4145 mL | 1.0362 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3454 mL | 0.8635 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2591 mL | 0.6476 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5181 mL |
Enrupatinib Related Classifications
HY-159838 Related Classifications
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