BPR1R024
Based on 1 Customer Validation
BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology.
For research use only. We do not sell to patients.
- Purity: 98.50%
- CAS No.: 2503015-75-4
- Formula: C24H21F3N6O2
- Molecular Weight:482.46
-
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Membrane Protein-targeted Compound Library
HY-L149
-
Highly Selective Inhibitors Library
HY-L158
-
Cytokine Inhibitors Library
HY-L161
-
Macrophage Related Compound Library
HY-L174
-
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
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Biological Activity
IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB)[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | EC50 |
80 nM
Compound: 12; BPRIR024
|
Antiproliferative activity against mouse BaF3 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
Antiproliferative activity against mouse BaF3 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
|
[PMID: 34606263] |
| BMDM | IC50 |
0.031 μM
Compound: 12; BPRIR024
|
Growth inhibition of CSF1-induced mouse BMDM cell assessed as inhibition of M2 like macrophage growth incubated for 3 days by WST-8 assay
Growth inhibition of CSF1-induced mouse BMDM cell assessed as inhibition of M2 like macrophage growth incubated for 3 days by WST-8 assay
|
[PMID: 34606263] |
| BMDM | IC50 |
5.39 μM
Compound: 12; BPRIR024
|
Growth inhibition of CSF2-induced mouse BMDM cell assessed as inhibition of M1 like macrophage growth for 3 days by WST-8 assay
Growth inhibition of CSF2-induced mouse BMDM cell assessed as inhibition of M1 like macrophage growth for 3 days by WST-8 assay
|
[PMID: 34606263] |
| NFS-60 | EC50 |
95 nM
Compound: 12; BPRIR024
|
Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
Antiproliferative activity against mouse NFS-60 cells transfected with human ETV6-CSF1R assessed as reduction in cell viability measured after 72 hrs by MTS method
|
[PMID: 34606263] |
BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM[1].
BPR1R024 exhibits weake AURA and AURB inhibitory activity in enzyme activity assay with IC50 values of ＞10 μM and 1.40 μM, respeactively[1].
BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner[1].
BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-α production[1].
BPR1R024 (0-10 μM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:RAW264.7 and THP-1 cells
-
Concentration:0-500 nM
-
Incubation Time:16 h
-
Result:Significantly suppressed the CSF1R signal in a dose-dependent manner, at concentrations of approximately 50-75 and 1-10 nM in RAW264.7 and THP-1 cells, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Rats[1]
-
Dosage:5, 20, 25 mg/kg
-
Administration:IV, PO
-
Result:Exhibited high systemic drug exposure with the dose-normalized area under curve (DNAUC) values of 3635 ng/mL*h by the IV route and 362 ng/mL*h by the PO route and the modification increased oral bioavailability (F=35%).
-
Animal Model:C57BL/6 mice (six-week-old, male)[1]
-
Dosage:100 mg/kg
-
Administration:Oral, twice a day
-
Result:Delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio.
Chemical Information
-
CAS No. 2503015-75-4
-
Appearance Solid
-
Molecular Weight 482.46
-
Formula C24H21F3N6O2
-
Color Off-white to light yellow
-
SMILES
CN(C1=CC2=C(C(OC3=CC=C(C=C3)NC(NCC4=CC=C(N=C4)C(F)(F)F)=O)=NC=N2)C=C1)C
-
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 : 10 mg/mL (20.73 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)
Purity & Documentation
-
Data Sheet (272 KB)
-
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)
-
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 | 2.0727 mL | 10.3636 mL | 20.7271 mL | 51.8178 mL |
| 5 mM | 0.4145 mL | 2.0727 mL | 4.1454 mL | 10.3636 mL | |
| 10 mM | 0.2073 mL | 1.0364 mL | 2.0727 mL | 5.1818 mL | |
| 15 mM | 0.1382 mL | 0.6909 mL | 1.3818 mL | 3.4545 mL | |
| 20 mM | 0.1036 mL | 0.5182 mL | 1.0364 mL | 2.5909 mL |
BPR1R024 Related Classifications
HY-132935 Related Classifications
Powered by Bioz