Ki23057

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

MedKoo CAT#: 401517

CAS#: 516523-31-2

Description: Ki23057 is a a FGFR2 inhibitor, which enhances the chemosensitivity of drug-resistant gastric cancer cell lines when used in combination with chemotherapeutic drugs. Ki23057 might be therapeutically promising for treating drug-resistant gastric cancer cells, especially when used in combination with SN38, PTX, or VP16. The apoptosis process might be the main mechanism underlying the synergistic effect of these combinations. The ERCC1 and p53 genes may play an integral role in the synergism between Ki23057 and chemotherapeutic agents in drug-resistant cell lines. (source: Cancer Lett. 2011 Aug 1;307(1):47-52).

Chemical Structure

Ki23057

CAS# 516523-31-2

Instruction

Theoretical Analysis

MedKoo Cat#: 401517
Name: Ki23057
CAS#: 516523-31-2
Chemical Formula: C30H35N3O4
Exact Mass: 501.26
Molecular Weight: 501.617
Elemental Analysis: C, 71.83; H, 7.03; N, 8.38; O, 12.76

Price and Availability

Size	Price	Availability	Quantity
1g	USD -1
2g	USD -1
5g	USD -1
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: Ki23057; Ki-23057; Ki 23057.

IUPAC/Chemical Name: 2-((2-((4-(4-((4-(tert-butyl)phenyl)amino)phenoxy)-6-methoxyquinolin-7-yl)oxy)ethyl)amino)ethanol

InChi Key: VQCDZFWRGXFUMS-UHFFFAOYSA-N

InChi Code: InChI=1S/C30H35N3O4/c1-30(2,3)21-5-7-22(8-6-21)33-23-9-11-24(12-10-23)37-27-13-14-32-26-20-29(28(35-4)19-25(26)27)36-18-16-31-15-17-34/h5-14,19-20,31,33-34H,15-18H2,1-4H3

SMILES Code: COC1=C(OCCNCCO)C=C2N=CC=C(OC3=CC=C(NC4=CC=C(C(C)(C)C)C=C4)C=C3)C2=C1

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, not in water

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:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 501.62 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:
In vitro protocol:
In vivo protocol:

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1: Qiu H, Yashiro M, Zhang X, Miwa A, Hirakawa K. A FGFR2 inhibitor, Ki23057, enhances the chemosensitivity of drug-resistant gastric cancer cells. Cancer Lett. 2011 Aug 1;307(1):47-52. doi: 10.1016/j.canlet.2011.03.015. Epub 2011 Apr 8. PubMed PMID: 21482024.

2: Amano R, Yamada N, Doi Y, Yashiro M, Ohira M, Miwa A, Hirakawa K. Significance of keratinocyte growth factor receptor in the proliferation of biliary tract cancer. Anticancer Res. 2010 Oct;30(10):4115-21. PubMed PMID: 21036728.

3: Katoh M. Genetic alterations of FGF receptors: an emerging field in clinical cancer diagnostics and therapeutics. Expert Rev Anticancer Ther. 2010 Sep;10(9):1375-9. doi: 10.1586/era.10.128. PubMed PMID: 20836672.

4: Yashiro M, Shinto O, Nakamura K, Tendo M, Matsuoka T, Matsuzaki T, Kaizaki R, Ohira M, Miwa A, Hirakawa K. Effects of VEGFR-3 phosphorylation inhibitor on lymph node metastasis in an orthotopic diffuse-type gastric carcinoma model. Br J Cancer. 2009 Oct 6;101(7):1100-6. doi: 10.1038/sj.bjc.6605296. PubMed PMID: 19738610; PubMed Central PMCID: PMC2768106.

5: Yashiro M, Shinto O, Nakamura K, Tendo M, Matsuoka T, Matsuzaki T, Kaizaki R, Miwa A, Hirakawa K. Synergistic antitumor effects of FGFR2 inhibitor with 5-fluorouracil on scirrhous gastric carcinoma. Int J Cancer. 2010 Feb 15;126(4):1004-16. doi: 10.1002/ijc.24763. PubMed PMID: 19621385.

6: Katoh M. FGFR2 abnormalities underlie a spectrum of bone, skin, and cancer pathologies. J Invest Dermatol. 2009 Aug;129(8):1861-7. doi: 10.1038/jid.2009.97. Epub 2009 Apr 23. Review. PubMed PMID: 19387476.

7: Katoh Y, Katoh M. FGFR2-related pathogenesis and FGFR2-targeted therapeutics (Review). Int J Mol Med. 2009 Mar;23(3):307-11. Review. PubMed PMID: 19212647.

8: Sakurai K, Yamada N, Yashiro M, Matsuzaki T, Komatsu M, Ohira M, Miwa A, Hirakawa K. A novel angiogenesis inhibitor, Ki23057, is useful for preventing the progression of colon cancer and the spreading of cancer cells to the liver. Eur J Cancer. 2007 Nov;43(17):2612-20. Epub 2007 Oct 18. PubMed PMID: 17949968.

9: Nakamura K, Yashiro M, Matsuoka T, Tendo M, Shimizu T, Miwa A, Hirakawa K. A novel molecular targeting compound as K-samII/FGF-R2 phosphorylation inhibitor, Ki23057, for Scirrhous gastric cancer. Gastroenterology. 2006 Nov;131(5):1530-41. Epub 2006 Aug 22. PubMed PMID: 17101326.

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