1. Protein Tyrosine Kinase/RTK
  2. c-Fms
    VEGFR
    c-Kit
    PDGFR
  3. Ki20227

Ki20227 

Cat. No.: HY-10408 Purity: 99.17%
Handling Instructions

Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.

For research use only. We do not sell to patients.

Ki20227 Chemical Structure

Ki20227 Chemical Structure

CAS No. : 623142-96-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
2 mg USD 108 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 912 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

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Description

Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction[1].

IC50 & Target

IC50: 2 nM (CSF1R), 12 nM (VEGFR2), 451 nM (c-Kit) and 217 nM (PDGFRβ)[1]

In Vitro

Ki20227 (0.1-1000 nM; 72 hours) with 100 and 1,000 nM almost suppresses M-NFS-60 cell growth and HUVEC cell growth, respectively[1].
Ki20227 (0.1-1000 nM; 1 hour) suppresses M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner[1].

Cell Viability Assay[1]

Cell Line: M-NFS-60 cells, HUVEC cells, human A375 melanoma cells
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 72 hours
Result: 100 and 1,000 nM almost suppressed M-NFS-60 cell growth and HUVEC cell growth, respectively.

Cell Viability Assay[1]

Cell Line: RAW264.7 cell lysate
Concentration: 0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM
Incubation Time: 1 hour
Result: Suppressed M-CSF-dependent c-Fms phosphorylation in a dose-dependent manner.
In Vivo

Ki20227 (orally;10-50 mg/kg/d for 20 days) of 50 mg/kg/d of Ki20227 for 20 days markedly decreases the osteolytic lesion areas[1].
ki20227 during global ischemia led to a significant deficit in microglial density in the CNS in mice, and CSF1R-inhibition led to a significant reduction in the neuronal density of mice[2].

Animal Model: 4-week-old male F344/NJcl-rnu rats[1]
Dosage: 10, 20, and 50 mg/kg
Administration: Orally; once per day for 20 days
Result: Oral administration of 50 mg/kg/d markedly decreased the osteolytic lesion areas.
Molecular Weight

480.54

Formula

C₂₄H₂₄N₄O₅S

CAS No.

623142-96-1

SMILES

O=C(NC1=CC=C(C=C1OC)OC2=CC=NC3=CC(OC)=C(C=C23)OC)NC(C)C4=NC=CS4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (130.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0810 mL 10.4050 mL 20.8099 mL
5 mM 0.4162 mL 2.0810 mL 4.1620 mL
10 mM 0.2081 mL 1.0405 mL 2.0810 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.17 mg/mL (4.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.17 mg/mL (4.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.17 mg/mL (4.52 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Ki20227Ki 20227Ki-20227c-FmsVEGFRc-KitPDGFRCSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RVascular endothelial growth factor receptorSCFRCD117Platelet-derived growth factor receptorInhibitorinhibitorinhibit

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Ki20227
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