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R(+)XK469 inhibits hydroxylation of S-warfarin by CYP2C9.
Yong WP, Kim TW, Undevia SD, Innocenti F, Ratain MJ. Yong WP, et al. Eur J Cancer. 2009 Jul;45(11):1904-8. doi: 10.1016/j.ejca.2009.04.032. Epub 2009 May 21. Eur J Cancer. 2009. PMID: 19464879 Free PMC article.
RESULTS: R(+)XK469 competitively inhibited S-warfarin hydroxylation. The K(i) values of R(+)XK469 were estimated to be 959+/-426 microM for human liver microsomes and to be 377+/-92 microM for CYP2C9. CONCLUSION: At the recommended phase II dose of R(+)XK469, …
RESULTS: R(+)XK469 competitively inhibited S-warfarin hydroxylation. The K(i) values of R(+)XK469 were estimated to be 959+/-4 …
XK469, a topo IIbeta inhibitor, induces apoptosis in Waldenstrom's macroglobulinemia through multiple pathways.
Mensah-Osman E, Al-Katib A, Dandashi M, Mohammad R. Mensah-Osman E, et al. Int J Oncol. 2003 Dec;23(6):1637-44. Int J Oncol. 2003. PMID: 14612935
In this study, the apoptotic potential of XK469 and its mechanism in WSU-WM cell line was investigated. Exposure of WSU-WM cells to XK469 caused a decrease in viable cell number in a dose-dependent manner. In addition, XK469 caused the activation of caspase 3 …
In this study, the apoptotic potential of XK469 and its mechanism in WSU-WM cell line was investigated. Exposure of WSU-WM cells to …
XK469, a novel antitumor agent, inhibits signaling by the MEK/MAPK signaling pathway.
Lin H, Subramanian B, Nakeff A, Chen BD. Lin H, et al. Cancer Chemother Pharmacol. 2002 Apr;49(4):281-6. doi: 10.1007/s00280-002-0425-7. Epub 2002 Jan 24. Cancer Chemother Pharmacol. 2002. PMID: 11914906
XK469 was also able to block the activation of MEK by serum addition in starved U-937 cells. Exposure of cells to XK469 for 1 h was sufficient to inhibit the activation of MEK and its downstream kinase, MAPK. ...
XK469 was also able to block the activation of MEK by serum addition in starved U-937 cells. Exposure of cells to XK469 for 1 …
Preclinical antitumor activity of XK469 (NSC 656889).
LoRusso PM, Parchment R, Demchik L, Knight J, Polin L, Dzubow J, Behrens C, Harrison B, Trainor G, Corbett TH. LoRusso PM, et al. Invest New Drugs. 1998-1999;16(4):287-96. doi: 10.1023/a:1006206814025. Invest New Drugs. 1998. PMID: 10426660
XK469 (NSC 656889) is a water-soluble member of the novel quinoxaline family of antitumor agents. ...XK469 was efficacious both intravenously and orally. Regardless of dosing schedule, conventional mice tolerated higher total doses than SCID or nu/nu mice did. ...
XK469 (NSC 656889) is a water-soluble member of the novel quinoxaline family of antitumor agents. ...XK469 was efficacious bot …
XK469, a selective topoisomerase IIbeta poison.
Gao H, Huang KC, Yamasaki EF, Chan KK, Chohan L, Snapka RM. Gao H, et al. Proc Natl Acad Sci U S A. 1999 Oct 12;96(21):12168-73. doi: 10.1073/pnas.96.21.12168. Proc Natl Acad Sci U S A. 1999. PMID: 10518594 Free PMC article.
XK469 (NSC 697887) is a synthetic quinoxaline phenoxypropionic acid derivative that possesses unusual solid tumor selectivity and activity against multidrug-resistant cancer cells. We report here that XK469 and its S(-) and R(+)-isomers induce reversible protein-DNA …
XK469 (NSC 697887) is a synthetic quinoxaline phenoxypropionic acid derivative that possesses unusual solid tumor selectivity and act …
Metabolic profile of XK469 (2(R)-[4-(7-chloro-2-quinoxalinyl)oxyphenoxy]-propionic acid; NSC698215) in patients and in vitro: low potential for active or toxic metabolites or for drug-drug interactions.
Anderson LW, Collins JM, Klecker RW, Katki AG, Parchment RE, Boinpally RR, LoRusso PM, Ivy SP. Anderson LW, et al. Cancer Chemother Pharmacol. 2005 Oct;56(4):351-7. doi: 10.1007/s00280-004-0962-3. Epub 2005 May 13. Cancer Chemother Pharmacol. 2005. PMID: 15895233 Clinical Trial.
An oxidized product formed by cytosolic aldehyde oxidase was the predominant species both in urine and human hepatocytes in vitro. Conjugates of XK469 with glycine, taurine, and glucuronic acid, as well as the microsomal product, 4-oxo-XK469, were also found in urin …
An oxidized product formed by cytosolic aldehyde oxidase was the predominant species both in urine and human hepatocytes in vitro. Conjugate …
Mitotic arrest induced by XK469, a novel antitumor agent, is correlated with the inhibition of cyclin B1 ubiquitination.
Lin H, Liu XY, Subramanian B, Nakeff A, Valeriote F, Chen BD. Lin H, et al. Int J Cancer. 2002 Jan 1;97(1):121-8. doi: 10.1002/ijc.1570. Int J Cancer. 2002. PMID: 11774253 Free article.
XK469 (NSC 697887) is a novel antitumor agent with broad activity against a variety of tumors. ...Concentration-survival curves with continuous exposure indicated that XK469 had low cytotoxic activity against H116 cells. Cell cycle analysis revealed that XK469 …
XK469 (NSC 697887) is a novel antitumor agent with broad activity against a variety of tumors. ...Concentration-survival curves with …
Pro-apoptotic interactions between XK469 and the peripheral benzodiazepine receptor.
Kessel D, Horwitz JP. Kessel D, et al. Cancer Lett. 2001 Jul 26;168(2):141-4. doi: 10.1016/s0304-3835(01)00518-3. Cancer Lett. 2001. PMID: 11403918
XK469 (2-[4-(7-chloro-2-quinoxalinyloxy) phenoxy]propionic acid) is a new anti-tumor agent with substantial activity against several drug-resistant cell lines. Using murine leukemia L1210 cells in culture, we found the chiral R(+) form of XK469 to be substantially m …
XK469 (2-[4-(7-chloro-2-quinoxalinyloxy) phenoxy]propionic acid) is a new anti-tumor agent with substantial activity against several …
A pharmacogenetic study of aldehyde oxidase I in patients treated with XK469.
Ramírez J, Kim TW, Liu W, Myers JL, Mirkov S, Owzar K, Watson D, Mulkey F, Gamazon ER, Stock W, Undevia S, Innocenti F, Ratain MJ. Ramírez J, et al. Pharmacogenet Genomics. 2014 Feb;24(2):129-32. doi: 10.1097/FPC.0000000000000023. Pharmacogenet Genomics. 2014. PMID: 24300566 Free PMC article.
XK469 (NSC 697887) is a selective topoisomerase II beta inhibitor eliminated mainly by aldehyde oxidase I (AOX1). ...Our study provides a starting point for future investigations on the functionality of AOX1 SNPs. However, variability in XK469 clearance cannot be at …
XK469 (NSC 697887) is a selective topoisomerase II beta inhibitor eliminated mainly by aldehyde oxidase I (AOX1). ...Our study provid …
The quinoxaline anti-tumor agent (R+)XK469 inhibits neuroblastoma tumor growth.
Kakodkar NC, Peddinti R, Kletzel M, Tian Y, Guerrero LJ, Undevia SD, Geary D, Chlenski A, Yang Q, Salwen HR, Cohn SL. Kakodkar NC, et al. Pediatr Blood Cancer. 2011 Jan;56(1):164-7. doi: 10.1002/pbc.22639. Pediatr Blood Cancer. 2011. PMID: 20860039 Free PMC article.
The quinoxaline anti-tumor agent (R+)XK469 mediates its effects by topoisomerase IIB inhibition. This report describes a 14-year old with relapsed neuroblastoma who experienced disease stabilization for 14 months while receiving (R+)XK469 monotherapy. ...These precl …
The quinoxaline anti-tumor agent (R+)XK469 mediates its effects by topoisomerase IIB inhibition. This report describes a 14-year old …
57 results