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).
MedKoo Cat#: 401517
Name: Ki23057
CAS#: 516523-31-2
Chemical Formula: C30H35N3O4
Exact Mass: 501.26276
Molecular Weight: 501.6166
Elemental Analysis: C, 71.83; H, 7.03; N, 8.38; O, 12.76
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
The following data is based on the product molecular weight 501.6166 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 |
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.
