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Cat. No.: HY-189731

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CSF1R-IN-28

CSF1R-IN-28 is an orally active CSF-1R inhibitor (IC₅₀ 17.2 nM). CSF1R-IN-28 inhibits AKT phosphorylation and reduces the production of inflammatory cytokines (TNF-α, IL-6, and IL-1β). CSF1R-IN-28 dose-dependently alleviates hind paw swelling and arthritis index, and improves histopathological joint damage in adjuvant-induced arthritis rats. CSF1R-IN-28 can be used for research on rheumatoid arthritis.

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CAS No.: 3121274-21-0
Formule: C₂₄H₂₂F₃N₃O₅
Masse moléculaire:489.44

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

CSF1R-IN-28 Chemical Structure

CAS No.: 3121274-21-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

IC₅₀ & Target

^[1]

IL-6

IL-1β

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Voir tous les produits spécifiques à Isoform TNF Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	GI50	10000 nM	GI50 > 10,000 nM against parental BaF3 cells assessed as proliferation inhibition after 48 hrs by CellCountingKit-8. GI50 > 10,000 nM against parental BaF3 cells assessed as proliferation inhibition after 48 hrs by CellCountingKit-8.	42721528

In Vitro

Anti-cancerInnate ImmunityCytokines & ChemokinesCytokines and ChemokinesOthers

Anti-cancer

CSF1R-IN-28 (48 h) selectively inhibits TEL-CSF1R-BaF3 proliferation with a GI₅₀ of 12.89 nM, while having no effect on parental BaF3 cells^[1].

Innate Immunity

Cytokines & Chemokines

CSF1R-IN-28 (0.1-1 μM) dose-dependently inhibits CSF-1-induced p-CSF1R and p-AKT in RAW264.7 macrophages, with significant inhibition at 1 μM^[1].
CSF1R-IN-28 (0.1-1 μM; 0.5-1 h) inhibits CSF-1-induced p-CSF1R and p-AKT in RAW264.7 macrophages by immunofluorescence^[1].

Innate Immunity

Cytokines and Chemokines

CSF1R-IN-28 (5-15 μM; 24 h) dose-dependently inhibits LPS-induced release of TNF-α, IL-6, and IL-1β in RAW264.7 macrophages^[1].

Others

CSF1R-IN-28 (Compound 11g) (1 h) inhibits CSF-1R kinase in a cell-free ADP-Glo assay (IC₅₀17.2 nM)^[1].
CSF1R-IN-28 (1 μM) showed >90% inhibition of CSF-1R, PDGFRβ, and KIT in a selectivity panel of 78 kinases, with lower inhibition of FLT3, DDR1, and KDR^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

TEL-CSF1R-BaF3 and parental BaF3 cells
Concentration:

Various concentrations
Incubation Time:

48 h
Result:

Inhibited TEL-CSF1R-BaF3 proliferation with GI₅₀ = 12.89 nM and showed no significant inhibitory effect on parental BaF3 cells (GI₅₀ > 10,000 nM).

Immunofluorescence^[1]

Cell Line:

RAW264.7 macrophages
Concentration:

0.1, 0.3, and 1 μM
Incubation Time:

0.5-1 h (11g with CSF1); 12 h at 4 °C (primary antibody); 1 h (secondary antibody)
Result:

Reversed CSF-1-induced p-CSF1R and p-AKT to varying degrees at 0.1, 0.3, and 1 μM.
Significantly inhibited p-CSF1R and p-AKT; at 1 μM, p-CSF1R inhibition was comparable to reference compound PLX3397.

ELISA Assay^[1]

Cell Line:

RAW264.7 macrophages
Concentration:

5, 10, 15 μM
Incubation Time:

24 h
Result:

Dose-dependently suppressed TNF-α, IL-6, and IL-1β production in RAW264.7 macrophages, with no obvious cytotoxicity.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	V_z	CL	F
Rat^[1]	1 mg/kg	i.v.	0.81 h	0.033 h	520 ng/mL	240 ng·h/mL	251 ng·h/mL	0.70 h	3518 mL/kg	4017 mL/h/kg	/
Rat^[1]	10 mg/kg	p.o.	1.36 h	2 h	154 ng/mL	631 ng·h/mL	659 ng·h/mL	3.10 h	30,198 mL/kg	15,445 mL/h/kg	26.2 %

In Vivo

Innate Immunity

CSF1R-IN-28 (10-40 mg/kg; p.o. (gavage); daily; day 12 to day 27) reduces adjuvant-induced arthritis in rats, decreasing hind paw swelling, arthritis index, joint inflammation, cartilage damage, and serum pro-inflammatory cytokines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (SD) (male)^[1]
Dosage:

10 mg/kg; 20 mg/kg; 40 mg/kg
Administration:

p.o. (gavage); daily; from day 12 to day 27
Result:

Decreased hind paw swelling and arthritis index dose-dependently on days 21, 24, and 27.
After 27 days of dosing, 11g at 40 mg/kg showed efficacy comparable to positive control MTX.
In HE-stained ankle joints, 11g reduced inflammatory cell infiltration, improved synovial structure, and limited pannus formation; semi-quantitative grading scores were lower in each 11g dose group (10, 20, 40 mg/kg) than in the AIA model group.
In Safranin O/Fast Green-stained sections, 11g dose-dependently relieved cartilage damage compared with the AIA model group by Mankin scoring.
In AIA rat serum, 11g inhibited TNF-α, IL-6, and IL-1β production in a concentration-dependent manner at 10, 20, and 40 mg/kg.

Related Protocols :

Chemical Information

CAS No. 3121274-21-0
Masse moléculaire 489.44
Formule C₂₄H₂₂F₃N₃O₅
SMILES

O=C(C1=CN=CO1)N2CCC(OC3=CC(NC(C4=CC=C(OC(F)(F)F)C=C4)=O)=CC=C3C)CC2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Xia Z, et al. Discovery of oxazole-capped 4-phenoxypiperidine CSF1R type II inhibitors with potent in vivo anti-rheumatoid arthritis activity. Bioorganic chemistry. 2026 Sep 08;182:110499.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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CSF1R-IN-28

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