2. Protein Tyrosine Kinase/RTK
  3. c-Fms
  4. BPR1R024 mesylate

BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 mesylate is the equivalent of BPR1R024.html" class="link-product" target="_blank"> 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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BPR1R024 mesylate Chemical Structure

BPR1R024 mesylate Chemical Structure

CAS No. : 2763365-40-6

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BPR1R024 mesylate Related Antibodies

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Description

BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 mesylate is the equivalent of BPR1R024.html" class="link-product" target="_blank"> 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[1].

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.

BPR1R024 mesylate Related Antibodies

Western Blot Analysis[1]

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.
In Vivo

BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model[1].

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.
Molecular Weight

578.56

Formula

C25H25F3N6O5S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BPR1R024 mesylate Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BPR1R0242763365-40-6c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1Roralcolony-stimulating factor-1 receptor (CSF1R)inhibitionimmuno-oncologyInhibitorinhibitorinhibit

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