200484-11-3 | Chs-828

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$28.00	$19.00
5mg	98%	in stock	$42.00	$30.00
10mg	98%	in stock	$51.00	$36.00
25mg	98%	in stock	$113.00	$79.00
250mg	98%	in stock	$298.00	$209.00

Description

• Catalog Number: AB09693
• Chemical Name: Chs-828
• CAS Number: 200484-11-3
• Molecular Formula: C19H22ClN5O
• Molecular Weight: 371.8639
• MDL Number: MFCD03700766
• SMILES: N#CNC(=Nc1ccncc1)NCCCCCCOc1ccc(cc1)Cl

Computed Properties

• Complexity: 450
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 26
• Hydrogen Bond Acceptor Count: 4
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 11
• XLogP3: 4.3

Literature

• Retinal toxicity, in vivo and in vitro, associated with inhibition of nicotinamide phosphoribosyltransferase.

  Toxicological sciences : an official journal of the Society of Toxicology 20150301

• Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner.

  The Journal of biological chemistry 20120622

• Reciprocal potentiation of the antitumoral activities of FK866, an inhibitor of nicotinamide phosphoribosyltransferase, and etoposide or cisplatin in neuroblastoma cells.

  The Journal of pharmacology and experimental therapeutics 20110901

• Safety and efficacy of NAD depleting cancer drugs: results of a phase I clinical trial of CHS 828 and overview of published data.

  Cancer chemotherapy and pharmacology 20100501

• Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase.

  BMC cancer 20100101

• Preclinical development of the nicotinamide phosphoribosyl transferase inhibitor prodrug GMX1777.

  Anti-cancer drugs 20090601

• Regression of orthotopic neuroblastoma in mice by targeting the endothelial and tumor cell compartments.

  Journal of translational medicine 20090101

• Anticancer agent CHS-828 inhibits cellular synthesis of NAD.

  Biochemical and biophysical research communications 20080321

• Ariad Pharmaceuticals wins first round over Eli Lilly, patents on methods can be far-reaching.

  Journal of the National Cancer Institute 20060802

• CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome.

  Anticancer research 20060101

• EB1627: a soluble prodrug of the potent anticancer cyanoguanidine CHS828.

  Bioorganic & medicinal chemistry letters 20050516

• Pharmacokinetic-pharmacodynamic modelling of the schedule-dependent effect of the anti-cancer agent CHS 828 in a rat hollow fibre model.

  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 20050501

• Phase I study and pharmacokinetic of CHS-828, a guanidino-containing compound, administered orally as a single dose every 3 weeks in solid tumours: an ECSG/EORTC study.

  European journal of cancer (Oxford, England : 1990) 20050301

• Antitumoural effects of the pyridyl cyanoguanidine CHS 828 on three different types of neuroendocrine tumours xenografted to nude mice.

  Neuroendocrinology 20050101

• Anticancer agent CHS 828 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity.

  International journal of cancer 20040820

• Multiparametric evaluation of apoptosis: effects of standard cytotoxic agents and the cyanoguanidine CHS 828.

  Molecular cancer therapeutics 20040501

• Synthesis and in vitro cytotoxicity of 5-substituted 2-cyanoimino-4-imidazodinone and 2-cyanoimino-4-pyrimidinone derivatives.

  Bioorganic & medicinal chemistry letters 20040308

• Development and characterization of two human tumor sublines expressing high-grade resistance to the cyanoguanidine CHS 828.

  Anti-cancer drugs 20040101

• Cytotoxic effect in vivo and in vitro of CHS 828 on human myeloma cell lines.

  Anti-cancer drugs 20040101

• Segmental analysis of molecular surface electrostatic potentials: application to enzyme inhibition.

  Journal of molecular modeling 20030401

• Activation of p53 protein in normal and in tumor cells by a novel anticancer agent CHS 828.

  Drugs under experimental and clinical research 20030101

• The combination of the antitumoural pyridyl cyanoguanidine CHS 828 and etoposide in vitro--from cytotoxic synergy to complete inhibition of apoptosis.

  British journal of pharmacology 20021001

• Interactions between the new cytotoxic drug CHS 828 and amiloride and mitomycin C in a human tumour cell line and in tumour cells from patients.

  Chemotherapy 20020901

• A Phase I study of CHS 828 in patients with solid tumor malignancy.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20020901

• Action of a novel anticancer agent, CHS 828, on mouse fibroblasts: increased sensitivity of cells lacking poly (ADP-Ribose) polymerase-1.

  Cancer research 20020801

• In vitro activity of the novel cytotoxic agent CHS 828 in childhood acute leukemia.

  Anti-cancer drugs 20020801

• CHS 828 inhibits neuroblastoma growth in mice alone and in combination with antiangiogenic drugs.

  Pediatric research 20020501

• Modulation of pyridyl cyanoguanidine (CHS 828) induced cytotoxicity by 3-aminobenzamide in U-937 GTB cells.

  Biochemical pharmacology 20020415

• Metabolic effects of the cytotoxic guanidino-containing drug CHS 828 in human U-937 lymphoma cells.

  Anticancer research 20020101

• Model for time dependency of cytotoxic effect of CHS 828 in vitro suggests two different mechanisms of action.

  The Journal of pharmacology and experimental therapeutics 20011201

• Activity of CHS 828 in primary cultures of human hematological and solid tumors in vitro.

  Anti-cancer drugs 20011101

• Guanidino-containing drugs in cancer chemotherapy: biochemical and clinical pharmacology.

  Biochemical pharmacology 20010515

• Cellular pharmacodynamics of the cytotoxic guanidino-containing drug CHS 828. Comparison with methylglyoxal-bis(guanylhydrazone).

  European journal of pharmacology 20010420

• Cell death with atypical features induced by the novel antitumoral drug CHS 828, in human U-937 GTB cells.

  European journal of pharmacology 20010413

• In vivo activity of CHS 828 on hollow-fibre cultures of primary human tumour cells from patients.

  Cancer letters 20010126

• Temporal effects of the novel antitumour pyridyl cyanoguanidine (CHS 828) on human lymphoma cells.

  European journal of cancer (Oxford, England : 1990) 20010101

• A hollow fiber model for in vitro studies of cytotoxic compounds: activity of the cyanoguanidine CHS 828.

  Anti-cancer drugs 20010101

• Rapid screening of Veillonella by ultraviolet fluorescence.

  Journal of clinical microbiology 19751201