BPR1R024 mesylate
BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology.
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- CAS No.: 2763365-40-6
- Formule: C25H25F3N6O5S
- Masse moléculaire:578.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
IC50 & Target
IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB)[1].
In Vitro
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. Further protocols information, click here.
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Cell Line:RAW264.7 and THP-1 cells
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Concentration:0-500 nM
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Incubation Time:16 h
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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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[1]
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Dosage:5, 20, 25 mg/kg
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Administration:IV, PO
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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%).
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Animal Model:C57BL/6 mice (six-week-old, male)[1]
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Dosage:100 mg/kg
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Administration:Oral, twice a day
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Result:Delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio.
Chemical Information
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CAS No. 2763365-40-6
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Masse moléculaire 578.56
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Formule C25H25F3N6O5S
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SMILES
OS(=O)(C)=O.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
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BPR1R024 mesylate Related Classifications
HY-132935A Related Classifications
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