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
- 화학식: C25H25F3N6O5S
- 분자량:578.56
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB)[1].
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.
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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.
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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분자량 578.56
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BPR1R024 mesylate Related Classifications
HY-132935A Related Classifications
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