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Chemical Structure| 623142-96-1 Chemical Structure| 623142-96-1

Structure of Ki20227
CAS No.: 623142-96-1

Chemical Structure| 623142-96-1

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Ki-20227 is a highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50 value of 2 nM, displaying 6 fold and > 100 fold selectivity over VEGFR2 (IC50=12 nM) and c-Kit/PDGFRβ (IC50=451/217 nM), respectively.

Synonyms: Ki20227

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Product Details of Ki20227

CAS No. :623142-96-1
Formula : C24H24N4O5S
M.W : 480.54
SMILES Code : O=C(NC(C1=NC=CS1)C)NC2=CC=C(OC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2OC
Synonyms :
Ki20227
MDL No. :MFCD12024693
InChI Key :SHPFDGWALWEPGS-UHFFFAOYSA-N
Pubchem ID :9869779

Safety of Ki20227

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Ki20227

RTK

Isoform Comparison

Biological Activity

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice LEC injection-induced osteolysis model Oral 40 mg/kg/day Once daily for 2 weeks To investigate the effect of Ki20227 on LEC-induced osteolysis, results showed that Ki20227 significantly reduced bone destruction. J Bone Miner Res. 2017 May;32(5):939-950
Mouse BAPN-induced thoracic aortic aneurysm and dissection model Oral 30 mg/kg Daily administration for 28 days Suppression of macrophage accumulation in the aorta significantly decreased the incidence of TAAD and aortic rupture in mice. Cell Discov. 2022 Feb 8;8(1):11
Mice Global cerebral ischemia model induced by bilateral common carotid artery ligation (BCAL) Intragastric administration 2 mg/kg/day Once daily for 3 days Ki20227 inhibition of CSF1R resulted in blockade of microglial proliferation and morphological changes, exacerbating neuronal degeneration and behavioral deficits. Front Cell Neurosci. 2020 Oct 16;14:267
C57BL/6 mice Ischemic stroke model Oral gavage 0.002 mg/kg/day Once daily for 7 or 14 days Ki20227 pretreatment improved neurobehavioral function in stroke mice, upregulated synaptic protein expressions and dendritic spine density, while downregulating Iba1 expression, indicating inhibition of CSF1R signaling and activation of BDNF and autophagic pathways Mediators Inflamm. 2020 Oct 31;2020:8796103
C57BL/6 male mice Cerebral ischemia stroke model Gavage 0.002 mg/kg/day 7 consecutive days, once daily Ki20227 pretreatment significantly reduced neurological scores, improved neurological impairment, reduced brain infarction volume, inhibited microglia M1 phenotype and activated M2 phenotype, and inhibited NLRP3 inflammasome and NLRP3 signaling pathway activation. Neural Plast. 2020 Aug 28;2020:8825954
Mice Spontaneous melanoma model Oral 30–40 mg/kg/day Daily administration for 4 to 6 weeks Postoperative use of Ki20227 significantly reduced tumor recurrence and inhibited metastatic growth Oncotarget. 2015 Sep 8;6(26):22857-68

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.40mL

2.08mL

1.04mL

20.81mL

4.16mL

2.08mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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