ArticleInvestigational new drugs
Preclinical antitumor activity of XK469 (NSC 656889).
Article in Investigational new drugs. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 56 citations in OpenAlex.
- Discovery of new thiadiazole-based VEGFR-2 inhibitors: design, synthesis, cytotoxicity, and apoptosis induction.Future medicinal chemistry · 2025Article
- Design and synthesis of thiadiazoles as anticancer, apoptotic, and VEGFR-2 inhibitors.Future medicinal chemistry · 2025Article
- Synthesis, In Vitro Antiproliferative Activity, and In Silico Evaluation of Novel Oxiranyl-Quinoxaline Derivatives.Pharmaceuticals (Basel, Switzerland) · 2022Article
- Synthesis of new quinoxalines containing an oxirane ring by the TDAE strategy and in vitro evaluation in neuroblastoma cell lines.Molecules (Basel, Switzerland) · 2014Article
- The quinoxaline anti-tumor agent (R+)XK469 inhibits neuroblastoma tumor growth.Pediatric blood & cancer · 2011Article
- R(+)XK469 inhibits hydroxylation of S-warfarin by CYP2C9.European journal of cancer (Oxford, England : 1990) · 2009Article
- A phase I and pharmacokinetic study of the quinoxaline antitumour Agent R(+)XK469 in patients with advanced solid tumours.European journal of cancer (Oxford, England : 1990) · 2008Article
- A phase I and pharmacokinetic study of XK469R (NSC 698215), a quinoxaline phenoxypropionic acid derivative, in patients with refractory acute leukemia.Investigational new drugs · 2008Article
- A phase 1 trial of XK469: toxicity profile of a selective topoisomerase IIbeta inhibitor.Investigational new drugs · 2007Article
- The role of autophagy in the death of L1210 leukemia cells initiated by the new antitumor agents, XK469 and SH80.Molecular cancer therapeutics · 2007Article
- Induction of apoptosis by the new anticancer drug XK469 in human ovarian cancer cell lines.Oncogene · 2002Article
- Lack of in vitro-in vivo correlation of a novel investigational anticancer agent, SH 30.Investigational new drugs · 2002Article
- Preclinical efficacy evaluations of XK-469: dose schedule, route and cross-resistance behavior in tumor bearing mice.Investigational new drugs · 2002Article
- Preclinical antitumor efficacy of analogs of XK469: sodium-(2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]propionate.Investigational new drugs · 1998Article
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 1 country.
Funding
Abstract
XK469 (NSC 656889) is a water-soluble member of the novel quinoxaline family of antitumor agents. In vitro, XK469 demonstrated selective cytotoxicity for several murine solid tumors including colorectal and mammary adenocarcinoma cell lines, when compared to both leukemia and normal epithelial cells. In vivo, XK469 was active against 7/7 murine tumors tested, including pancreatic ductal carcinomas #02 and #03, colon adenocarcinomas #38 and #51/A, mammary adenocarcinoma #16/C and the Adriamycin resistant mammary adenocarcinomas #16/C/ADR and #17/ADR. XK469 was efficacious both intravenously and orally. Regardless of dosing schedule, conventional mice tolerated higher total doses than SCID or nu/nu mice did. Despite these reduced doses, XK469 was active against xenografts of 4/6 human tumor lines including mammary adenocarcinoma MX-1, the small cell lung cancer DMS 273, the prostate model LNCaP and the CNS tumor SF295. The lower doses in the xenograft studies were below curative levels. The dose-limiting toxicity appeared to be myelosuppression with rapid host recovery (5-8 days), and in vitro assays of XK469 toxicity to murine bone marrow neutrophil progenitors CFU-GM (colony forming unit-granulocyte/macrophage) demonstrated concentration-dependent toxicity from 0.5-30 microg/mL. The difference in drug tolerance between BDF1 and SCID mice was detected in vitro as a 3-fold difference in the IC90 for CFU-GM, despite similar IC50 values. Comparative in vitro hematotoxicology studies revealed that human bone marrow CFU-GM tolerated XK469 as well as their SCID counterparts (IC90 values 5.7 vs. 7.4 microg/mL). Based on comparison with previously tested anti-cancer agents, these data suggest that humans will be able to tolerate XK469 doses that are efficacious against human tumor xenografts.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.