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Art. -Nr.: HY-155001

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CSF1R-IN-15

CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages.

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CAS. Nr.: 2925744-43-8
Formel: C₂₂H₂₂N₄O
Molecular Weight:358.44

Speicherung:

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

Data Sheet (271 KB)

CSF1R-IN-15 Chemical Structure

CAS. Nr.: 2925744-43-8

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>9.9 μM Compound: 27g	Cytotoxicity against IL-3-dependent mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay Cytotoxicity against IL-3-dependent mouse BaF3 cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay	[PMID: 38141285]

In Vitro

CSF1R-IN-15 (0.007-10 μM, 72 h) is inactive to Ba/F3 cell viability, while Pex significantly (HY-16749) showed superior activity ^[1].
CSF1R-IN-15 assessment of plasma protein binding is measured by equilibrium dialysis. CSF1R-IN-15 (5 μM, 6 h, 37 °C) was incubated with plasma and showed 69% binding to mouse plasma proteins^[1].
Pharmacokinetic Analysis for CSF1R-IN-15 (compound 23) in vitro^[1]

HLM CL_int(μL/min/mg)	HLM CL_int(μL/min/mg)	HLM CL_int(μL/min/mg)	Plasmastab.	PPB
15.5	40	86	69	94

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3-hCSF1R Cells
Concentration:

0.007-10 μM
Incubation Time:

72 h
Result:

Exhibited no activity while pexidartinib (HY-16749) has superior activity.

In Vivo

In vivo pharmacokinetic indices were derived from cassette dosing studies. The t_1/2, C₀, AUC_0-∞, CL_obs, and V_ss,obs of CSF1R-IN-15 were 0.5 h, 37 ng/mL, 18 h*ng/mL, 54 L/h/kg, and 32 L/kg in C57BLKS mice^[1].
Pharmacokinetic Analysis in CSF1R-IN-15 (compound 23) for a cassette dosing study in C57BLKS mice^[1]

t_1/2 (h)	C₀ (ng/mL)	AUC_0-∞ (h*ng/mL)	CL_obs (L/h/kg)	V_ss,obs (L/kg)
0.5	37	18	54	32

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

Animal Model:

In Vivo Pharmacokinetic Study
Dosage:

1mg/kg
Administration:

Intravenous injection (i.v.) single dosing of drugs (1 mg/kg each) in a 20% DMSO, 80% PEG400 formulation. Blood sampling was done after 10, 30, 60, 120, 240, and 480 min.
Result:

In vivo pharmacokinetic indexes were t_1/2 (0.5 h), C₀ (37 ng/mL), AUC_0-∞ (18 h*ng/mL), CL_obs (54 L/h/kg), and V_ss,obs (32 L/kg), respectively.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

Chemical Information

CAS. Nr. 2925744-43-8
Molecular Weight 358.44
Formel C₂₂H₂₂N₄O
SMILES

CN(C1=NC=NC2=C1C=C(N2)C3=CC=C(C=C3)CO)CC4=CC=CC(C)=C4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Aarhus TI, et al. Synthesis and Development of Highly Selective Pyrrolo[2,3-d]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form. J Med Chem. 2023 May 25;66(10):6959-6980. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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