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Chloroquinoxaline sulfonamide Sale

(Synonyms: 4-氨基-N-(5-氯-2-喹喔啉)苯磺酰胺,Chloroquinoxaline; NSC-339004) 目录号 : GC60107

Chloroquinoxaline sulfonamide (Chloroquinoxaline) 是 sulfaquinoxaline 的结构类似物,是拓扑异构酶 II alpha/beta (topoisomerase II alpha/beta) 毒物。Chloroquinoxaline sulfonamide 用于控制家禽,兔,绵羊和牛的球虫病。 具有抗肿瘤活性。

Chloroquinoxaline sulfonamide Chemical Structure

Cas No.:97919-22-7

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10mM (in 1mL DMSO)
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1mg
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50mg
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产品描述

Chloroquinoxaline sulfonamide (Chloroquinoxaline), a structural analogue of sulfaquinoxaline, is a topoisomerase II alpha/beta poison. Chloroquinoxaline sulfonamide is used to control coccidiosis in poultry, rabbit, sheep, and cattle[1]. Antitumor activity[2].

The Chloroquinoxaline sulfonamide IC50 for CV-1cells, obtained using an MTT cytotoxicity assay, was 1.8 mM. Chloroquinoxaline sulfonamide causes dose-dependent protein-DNA cross-links to CV-1 monkey kidney cell chromosomal DNA when drug treatment was terminated by lysis with GuHCl. Chloroquinoxaline sulfonamide-induced protein-DNA cross-links in CV-1 cells. Chloroquinoxaline sulfonamide-induced topoisomerase II-DNA cross-links[1].Chloroquinoxaline sulfonamide (Chloroquinoxaline), a chlorinated derivative of sulfaquinoxaline, inhibits proliferation of murine B16 melanoma cells, but only when relatively high drug concentrations (1 mM) are used[2]. Cell Proliferation Assay[2] Cell Line: B16 murine melanoma cells

[1]. Gao H, et al. Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison. Cancer Res. 2000 Nov 1;60(21):5937-40. [2]. Branda RF, et al. Cellular pharmacology of chloroquinoxaline sulfonamide and a related compound in murine B16 melanoma cells. Biochem Pharmacol. 1988 Dec 1;37(23):4557-64.

Chemical Properties

Cas No. 97919-22-7 SDF
别名 4-氨基-N-(5-氯-2-喹喔啉)苯磺酰胺,Chloroquinoxaline; NSC-339004
Canonical SMILES ClC1=CC=CC2=NC(NS(=O)(C3=CC=C(N)C=C3)=O)=CN=C12
分子式 C14H11ClN4O2S 分子量 334.78
溶解度 DMSO: 125 mg/mL (373.38 mM) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.987 mL 14.9352 mL 29.8704 mL
5 mM 0.5974 mL 2.987 mL 5.9741 mL
10 mM 0.2987 mL 1.4935 mL 2.987 mL
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Research Update

Chloroquinoxaline sulfonamide: a sulfanilamide antitumor agent entering clinical trials

Invest New Drugs 1993 Feb;11(1):1-9.PMID:8349430DOI:10.1007/BF00873904.

Chloroquinoxaline sulfonamide (CQS) has been developed to the clinical trial stage based on its activity in the Human Tumor Colony Forming Assay (HTCFA). In the HTCFA, CQS demonstrated inhibition of colony formation against breast, lung, melanoma and ovarian carcinomas. The mechanism of action of CQS is unknown. It does not appear to inhibit folate metabolism as does the structurally similar sulfaquinoxaline. Preclinical toxicology studies in dogs and rats have shown that CQS is toxic to lymphoid organs, bone marrow, gastrointestinal tract, pancreas, CNS, adrenal glands and testes. Toxicity was generally reversible with the exception of testicular atrophy in dogs and rats which occurred late and was not reversible within the study time frame. The pharmacokinetic data indicate that CQS binds to serum proteins in a dose and species specific manner. Terminal half-lives appear to vary between species from 60 hours in mice, 15 hours in rats, and 45-132 hours in dogs. Preliminary data indicate a longer terminal half-life in humans. Two phase I trials are ongoing using a 60 min infusion schedule once every 28 days. The starting dose for each trial was 18 mg/m2.

Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15

Science 2017 Apr 28;356(6336):eaal3755.PMID:28302793DOI:10.1126/science.aal3755.

Indisulam is an aryl sulfonamide drug with selective anticancer activity. Its mechanism of action and the basis for its selectivity have so far been unknown. Here we show that indisulam promotes the recruitment of RBM39 (RNA binding motif protein 39) to the CUL4-DCAF15 E3 ubiquitin ligase, leading to RBM39 polyubiquitination and proteasomal degradation. Mutations in RBM39 that prevent its recruitment to CUL4-DCAF15 increase RBM39 stability and confer resistance to indisulam's cytotoxicity. RBM39 associates with precursor messenger RNA (pre-mRNA) splicing factors, and inactivation of RBM39 by indisulam causes aberrant pre-mRNA splicing. Many cancer cell lines derived from hematopoietic and lymphoid lineages are sensitive to indisulam, and their sensitivity correlates with DCAF15 expression levels. Two other clinically tested sulfonamides, tasisulam and Chloroquinoxaline sulfonamide, share the same mechanism of action as indisulam. We propose that DCAF15 expression may be a useful biomarker to guide clinical trials of this class of drugs, which we refer to as SPLAMs (splicing inhibitor sulfonamides).

Chloroquinoxaline sulfonamide (NSC 339004) is a topoisomerase IIalpha/beta poison

Cancer Res 2000 Nov 1;60(21):5937-40.PMID:11085507doi

Chloroquinoxaline sulfonamide (chlorosulfaquinoxaline, CQS, NSC 339004) is active against murine and human solid tumors. On the basis of its structural similarity to the topoisomerase IIbeta-specific drug XK469, CQS was tested and found to be both a topoisomerase-IIalpha and a topoisomerase-IIbeta poison. Topoisomerase II poisoning by CQS is essentially undetectable in assays using the common protein denaturant SDS, but easily detectable with strong chaotropic protein denaturants. The finding that detection of topoisomerase poisoning can be so dependent on the protein denaturant used in the assay has implications for drug discovery efforts and for our understanding of topoisomerase poisons.

Immunosuppressive properties of Chloroquinoxaline sulfonamide

Biochem Pharmacol 1989 Oct 15;38(20):3521-6.PMID:2818644DOI:10.1016/0006-2952(89)90123-8.

Chloroquinoxaline sulfonamide (CQS), a sulfanilamide derivative with antitumor activity, was found to be toxic to lymphoid tissue during preclinical studies. The mechanism of this toxicity appears to involve profound inhibition of lymphocyte activation. Incubation of human peripheral blood mononuclear cells (PBMNCs) with CQS decreased cellular incorporation of thymidine and deoxyuridine in a dose-dependent manner. Analysis of cell cycle distribution by flow cytometry indicated that CQS blocked movement out of the G0/G1 phase. Drug-treated cells were smaller and expressed fewer receptors for interleukin-2 (IL-2) and transferrin than untreated mitogen-stimulated lymphocytes. These observations support the notion that CQS has cell cycle specificity in regulating lymphocyte proliferation. As little as 10 microM CQS markedly inhibited both human lymphocyte and murine CTLL cell replication in response to IL-2 containing growth factors. However, CQS did not block secretion of IL-2 into culture supernatant fractions by human PBMNCs. Finally, CQS inhibited in vitro production of immunoglobulins G and M by mitogen-stimulated lymphocytes, primarily by causing cytotoxicity. In all of these drug effects, CQS was approximately one to two logs more potent than the parent compound, sulfaquinoxaline (SQ). These studies indicate that CQS inhibits essential basic processes in human lymphocytes. This agent may find use as an immunosuppressive drug.

A phase II study of Chloroquinoxaline sulfonamide (CQS) in patients with metastatic colorectal carcinoma (MCRC)

Invest New Drugs 2006 Jul;24(4):343-6.PMID:16446986DOI:10.1007/s10637-005-4827-3.

Purpose: Phase II multicenter study investigated the efficacy and toxicity of the novel halogenated derivative of sulfaquixonaline Chloroquinoxaline sulfonamide (CQS) in metastatic colorectal cancer. Experimental design: Eligible patients with metastatic or recurrent colorectal cancer received CQS at a dose schedule of 2000 mg/m2 over an hour weekly for 4 weeks every 42 days. Treatment was continued until unexpected toxicity or disease progression. Results: A total of seventeen patients were enrolled on this study. 94% of all patients enrolled had prior treatment. Sixteen patients were evaluable for response with fifteen patients showing evidence of disease progression and one patient with prolonged stable disease. One patient had non-evaluable disease. Following this interim analysis, the drug was considered ineffective and the study was terminated early. The most frequent adverse event was anemia. No patients discontinued the treatment because of toxicity. Conclusion: CQS, when given at a dose of 2000 mg/m2 weekly for 4 weeks every 42 days to patients with metastatic colorectal cancer, does not result in significant tumor regression.