KI-20227


Catalog No. size PriceQuantity
M6532-2 2mg solid $125
M6532-10 10mg solid $535

Description

Cas:623142-96-1

Product Information:

KI-20227 is a potent and orally active inhibitor of c-Fms tyrosine kinase (M-CSFR, CSF1R) (IC50 values are 2, 12, 217 and 451 nM for c-Fms, VEGFR-2, PDGFRβ and c-Kit respectively). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Ki20227 inhibits disease progression in a collagen-induced arthritis mouse model. Ki20227 suppresses experimental autoimmune encephalomyelitis.

 

Chemical Formula: C24H24N4O5S

 

Exact Mass: 480.1467

 

Molecular Weight: 480.539

 

Elemental Analysis: C, 59.99; H, 5.03; N, 11.66; O, 16.65; S, 6.67

 

Synonym:

 

KI-20227

KI 20227

KI20227

 

Chemical Name: 

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

 

InChi Key:

SHPFDGWALWEPGS-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C24H24N4O5S/c1-14(23-26-9-10-34-23)27-24(29)28-17-6-5-15(11-20(17)30-2)33-19-7-8-25-18-13-22(32-4)21(31-3)12-16(18)19/h5-14H,1-4H3,(H2,27,28,29)

 

Smiles Code:

O=C(NC(C1=NC=CS1)C)NC2=CC=C(OC3=CC=NC4=CC(OC)=C(OC)C=C34)C=C2OC

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

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.

Ki20227 (0.1-1000 nM; 1 hour) suppresses 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.

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.

 

 

References:

 

  1. Aikawa Y, Yamagata K, Katsumoto T, Shima Y, Shino M, Stanley ER, Cleary ML, Akashi K, Tenen DG, Kitabayashi I. Essential role of PU.1 in maintenance of mixed lineage leukemia-associated leukemic stem cells. Cancer Sci. 2015 Mar;106(3):227-36. doi: 10.1111/cas.12593. Epub 2015 Feb 12. PubMed PMID: 25529853; PubMed Central PMCID: PMC4373983.

 

  1. Toy EP, Lamb T, Azodi M, Roy WJ, Woo HH, Chambers SK. Inhibition of the c-fms proto-oncogene autocrine loop and tumor phenotype in glucocorticoid stimulated human breast carcinoma cells. Breast Cancer Res Treat. 2011 Sep;129(2):411-9. doi: 10.1007/s10549-010-1247-7. Epub 2010 Nov 10. PubMed PMID: 21063905.

 

  1. Uemura Y, Ohno H, Ohzeki Y, Takanashi H, Murooka H, Kubo K, Serizawa I. The selective M-CSF receptor tyrosine kinase inhibitor Ki20227 suppresses experimental autoimmune encephalomyelitis. J Neuroimmunol. 2008 Mar;195(1-2):73-80. doi: 10.1016/j.jneuroim.2008.01.015. Epub 2008 Apr 2. PubMed PMID: 18378004.

 

  1. Ohno H, Uemura Y, Murooka H, Takanashi H, Tokieda T, Ohzeki Y, Kubo K, Serizawa I. 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. PubMed PMID: 18085662.

 

  1. Ohno H, Kubo K, Murooka H, Kobayashi Y, Nishitoba T, Shibuya M, Yoneda T, Isoe T. 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. PubMed PMID: 17121910.

 

Products are for research use only. Not for human use.

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