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

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.

BPR1R024 Chemical Structure

BPR1R024 Chemical Structure

CAS No. : 2503015-75-4

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Based on 1 publication(s) in Google Scholar

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BPR1R024 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB)[1].
Cellular Effect
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]
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 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

482.46

Formula

C24H21F3N6O2
CAS No.
Appearance

Solid

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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0727 mL 10.3636 mL 20.7271 mL
5 mM 0.4145 mL 2.0727 mL 4.1454 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Animal weight
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g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.06%

SDS (251 KB)

COA (246 KB) HNMR (142 KB) RP-HPLC (138 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
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BPR1R024 Related Classifications

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:

BPR1R0242503015-75-4c-FmsCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1Roralcolony-stimulating factor-1 receptor (CSF1R)inhibitionimmuno-oncologyInhibitorinhibitorinhibit

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