Ki-20227 | Ki20227 | CAS#623142-96-1

KI-20227
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526787

CAS#: 623142-96-1

Description: 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 Structure

KI-20227

CAS# 623142-96-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526787
Name: KI-20227
CAS#: 623142-96-1
Chemical Formula: C24H24N4O5S
Exact Mass: 480.15
Molecular Weight: 480.539
Elemental Analysis: C, 59.99; H, 5.03; N, 11.66; O, 16.65; S, 6.67

Price and Availability

Size	Price	Availability
5mg	USD 320	2 Weeks
10mg	USD 550	2 Weeks
25mg	USD 990
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: KI-20227; KI 20227; KI20227.

IUPAC/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

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

More Info:

Product Data:

Product Data

Instruction:

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Biological target:	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.
In vitro activity:	Ki20227 inhibited M-CSF-dependent reactions, such as lipopolysaccharide-induced tumor necrosis factor-alpha production, which were enhanced by M-CSF in vitro. Reference: Eur J Immunol. 2008 Jan;38(1):283-91. https://pubmed.ncbi.nlm.nih.gov/18085662/
In vivo activity:	TP (triptolide) and Ki20227 pretreatments improved the neurobehavioral function in stroke mice. Synaptic protein expressions and density of dendritic spine density were upregulated in Ki20227 and TP pretreated stroke mice. Further, optimized integration of TP and Ki20227 pretreatments upregulated the NeuN expression and downregulated Iba1 expression after stroke. Reference: Mediators Inflamm. 2020 Oct 31;2020:8796103. https://pubmed.ncbi.nlm.nih.gov/33192177/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	12.5	26.01
	DMSO	54.8	113.96
	DMSO:PBS (pH 7.2) (1:3)	0.3	0.52
	Ethanol	3.0	6.24

Preparing Stock Solutions

The following data is based on the product molecular weight 480.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	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. doi: 10.1002/eji.200737199. PMID: 18085662. 2. 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. doi: 10.1158/1535-7163.MCT-05-0313. PMID: 17121910. 3. Du X, Gao F, Chen S, Botchway BOA, Amin N, Hu Z, Fang M. Combinational Pretreatment of Colony-Stimulating Factor 1 Receptor Inhibitor and Triptolide Upregulates BDNF-Akt and Autophagic Pathways to Improve Cerebral Ischemia. Mediators Inflamm. 2020 Oct 31;2020:8796103. doi: 10.1155/2020/8796103. PMID: 33192177; PMCID: PMC7648715. 4. Du X, Xu Y, Chen S, Fang M. Inhibited CSF1R Alleviates Ischemia Injury via Inhibition of Microglia M1 Polarization and NLRP3 Pathway. Neural Plast. 2020 Aug 28;2020:8825954. doi: 10.1155/2020/8825954. PMID: 32908485; PMCID: PMC7474788.
In vitro protocol:	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. doi: 10.1002/eji.200737199. PMID: 18085662. 2. 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. doi: 10.1158/1535-7163.MCT-05-0313. PMID: 17121910.
In vivo protocol:	1. Du X, Gao F, Chen S, Botchway BOA, Amin N, Hu Z, Fang M. Combinational Pretreatment of Colony-Stimulating Factor 1 Receptor Inhibitor and Triptolide Upregulates BDNF-Akt and Autophagic Pathways to Improve Cerebral Ischemia. Mediators Inflamm. 2020 Oct 31;2020:8796103. doi: 10.1155/2020/8796103. PMID: 33192177; PMCID: PMC7648715. 2. Du X, Xu Y, Chen S, Fang M. Inhibited CSF1R Alleviates Ischemia Injury via Inhibition of Microglia M1 Polarization and NLRP3 Pathway. Neural Plast. 2020 Aug 28;2020:8825954. doi: 10.1155/2020/8825954. PMID: 32908485; PMCID: PMC7474788.

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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.

2: 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.

3: 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.

4: 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.

5: 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.

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