| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:CSF1R-IN-15 CAS:2925744-43-8 Package:50mg/RMB 13800
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| | CSF1R-IN-15 Basic information |
| Product Name: | CSF1R-IN-15 | | Synonyms: | CSF1R-IN-15;Benzenemethanol, 4-[4-[methyl[(3-methylphenyl)methyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-6-yl]- | | CAS: | 2925744-43-8 | | MF: | C22H22N4O | | MW: | 358.44 | | EINECS: | | | Product Categories: | | | Mol File: | 2925744-43-8.mol |  |
| | CSF1R-IN-15 Chemical Properties |
| density | 1.269±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 12.935±0.50(predicted) |
| | CSF1R-IN-15 Usage And Synthesis |
| Uses | 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[1]. | | in vivo | In vivo pharmacokinetic indices were derived from cassette dosing studies. The t1/2, C0, AUC0-∞, CLobs, and Vss,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]
| t1/2 (h) | C0 (ng/mL) | AUC0-∞ (h*ng/mL) | CLobs (L/h/kg) | Vss,obs (L/kg) | | 0.5 | 37 | 18 | 54 | 32 |
| 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 t1/2 (0.5 h), C0 (37 ng/mL), AUC0-∞ (18 h*ng/mL), CLobs (54 L/h/kg), and Vss,obs (32 L/kg), respectively.
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| | References | [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. DOI:10.1021/acs.jmedchem.3c00428 |
| | CSF1R-IN-15 Preparation Products And Raw materials |
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