CAS 623142-96-1|Ki20227

Introduction：Basic information about CAS 623142-96-1|Ki20227, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Ki20227 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	Ki20227
CAS Number	623142-96-1	Molecular Weight	480.536
Density	1.3±0.1 g/cm3	Boiling Point	621.8±55.0 °C at 760 mmHg
Molecular Formula	C₂₄H₂₄N₄O₅S	Melting Point	/
MSDS	/	Flash Point	329.8±31.5 °C

Names

Name	1-[4-(6,7-dimethoxyquinolin-4-yl)oxy-2-methoxyphenyl]-3-[1-(1,3-thiazol-2-yl)ethyl]urea
Synonym	More Synonyms

Ki20227 BiologicalActivity

Description	Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFRβ(IC50=451/217 nM), respectively.IC50 value: Target: CSF1Rin vitro: Ki20227 did not inhibit other kinases tested, such as fms-like tyrosine kinase-3, epidermal growth factor receptor, or c-Src (c-src proto-oncogene product). Ki20227 was also found to inhibit the M-CSF-dependent growth of M-NFS-60 cells but not the M-CSF-independent growth of A375 human melanoma cells in vitro [1]. Ki20227 inhibited M-CSF-dependent reactions, such as lipopolysaccharide-induced tumor necrosis factor-alpha production, which were enhanced by M-CSF in vitro [2]. in vivo: Ki20227 decreased the number of tartrate-resistant acid phosphatase-positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats [1]. In addition, the number of CD11b(+), Gr-1(+), and Ly-6G(+) cells in the spleen decreased in the Ki20227-treated mice, and the CII-induced cytokine production in splenocytes isolated from the Ki20227-treated arthritic mice was also reduced [2]. Ki20227 treatments inhibited the turn-over/expansion of myeloid cells provoked by the immunization and subsequent MOG-specific T cell responses in our EAE animal model [3].
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-FmsResearch Areas >>Inflammation/Immunology
References	[1]. Ohno H, et al. A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006 Nov;5(11):2634-43. [2]. Ohno H, et al. The orally-active and selective c-Fms tyrosine kinase inhibitor Ki20227 inhibits disease progression in a collagen-induced arthritis mouse model. Eur J Immunol. 2008 Jan;38(1):283-91. [3]. Uemura Y, et al. The selective M-CSF receptor tyrosine kinase inhibitor Ki20227 suppresses experimental autoimmune encephalomyelitis. J Neuroimmunol. 2008 Mar;195(1-2):73-80. [4]. Boru Hou, et al. Ki20227 influences the morphology of microglia and neurons through inhibition of CSF1R during global ischemia. Int J Clin Exp Pathol. 2016;9(12):12459-12469.

Description

Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor with IC50 value of 2 nM; 6 fold and > 100 fold selectivity over VEGFR2(IC50=12 nM) and c-Kit/PDGFRβ(IC50=451/217 nM), respectively.IC50 value: Target: CSF1Rin vitro: Ki20227 did not inhibit other kinases tested, such as fms-like tyrosine kinase-3, epidermal growth factor receptor, or c-Src (c-src proto-oncogene product). Ki20227 was also found to inhibit the M-CSF-dependent growth of M-NFS-60 cells but not the M-CSF-independent growth of A375 human melanoma cells in vitro [1]. Ki20227 inhibited M-CSF-dependent reactions, such as lipopolysaccharide-induced tumor necrosis factor-alpha production, which were enhanced by M-CSF in vitro [2]. in vivo: Ki20227 decreased the number of tartrate-resistant acid phosphatase-positive osteoclast-like cells on bone surfaces in ovariectomized (ovx) rats [1]. In addition, the number of CD11b(+), Gr-1(+), and Ly-6G(+) cells in the spleen decreased in the Ki20227-treated mice, and the CII-induced cytokine production in splenocytes isolated from the Ki20227-treated arthritic mice was also reduced [2]. Ki20227 treatments inhibited the turn-over/expansion of myeloid cells provoked by the immunization and subsequent MOG-specific T cell responses in our EAE animal model [3].

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-FmsResearch Areas >>Inflammation/Immunology

References

[1]. Ohno H, et al. A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006 Nov;5(11):2634-43.

[2]. Ohno H, et al. The orally-active and selective c-Fms tyrosine kinase inhibitor Ki20227 inhibits disease progression in a collagen-induced arthritis mouse model. Eur J Immunol. 2008 Jan;38(1):283-91.

[3]. Uemura Y, et al. The selective M-CSF receptor tyrosine kinase inhibitor Ki20227 suppresses experimental autoimmune encephalomyelitis. J Neuroimmunol. 2008 Mar;195(1-2):73-80.

[4]. Boru Hou, et al. Ki20227 influences the morphology of microglia and neurons through inhibition of CSF1R during global ischemia. Int J Clin Exp Pathol. 2016;9(12):12459-12469.

Chemical & Physical Properties

Density	1.3±0.1 g/cm3
Boiling Point	621.8±55.0 °C at 760 mmHg
Molecular Formula	C₂₄H₂₄N₄O₅S
Molecular Weight	480.536
Flash Point	329.8±31.5 °C
Exact Mass	480.146729
PSA	132.07000
LogP	4.18
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.651
InChIKey	SHPFDGWALWEPGS-UHFFFAOYSA-N
SMILES	COc1cc(Oc2ccnc3cc(OC)c(OC)cc23)ccc1NC(=O)NC(C)c1nccs1
Storage condition	2-8℃

Synonyms

1-{4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl}-3-[1-(1,3-thiazol-2-yl)ethyl]urea

hms3244k11

hms3244l11

hms3244k12

Urea, N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N'-[1-(2-thiazolyl)ethyl]-

N-(4-((6,7-dimethoxy-4-quinolyl)oxy)-2-methoxyphenyl)-N'-(1-(1,3-thiazole-2-yl)ethyl)urea

Ki20227

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