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Rafoxanide

Catalog No. T7093   CAS 22662-39-1

Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.

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Rafoxanide Chemical Structure
Rafoxanide, CAS 22662-39-1
Pack Size Availability Price/USD Quantity
500 mg In stock $ 54.00
1 g In stock $ 85.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 100%
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Biological Description
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Description Rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer. Rafoxanide is a salicylanilide used as an anthelmintic. It is used to treat fluke, hookworm and other infestations.
In vitro Rafoxanide exhibit a high cytotoxic effects (IC50: 1.09 μM for A375 and 1.31 μM for A431 cells).?Consistent with the expected properties of CDK4/6 inhibitors, rafoxanide significantly increased the G1 phase population.?Notably, Rafoxanide specifically decreased the expression of CDK4/6, cyclin D, retinoblastoma protein (Rb) and the phosphorylation of CDK4/6 and Rb[1].
In vivo Rafoxanide specifically decreased the expression of CDK4/6, cyclin D, retinoblastoma protein (Rb) and the phosphorylation of CDK4/6 and Rb. Furthermore, the anticancer effect of rafoxanide was demonstrated in vivo in BALB/C nude mice subcutaneously xenografted with human skin cancer A375 cells. Rafoxanide (40 mg/kg, i.p.) exhibited significant antitumor activity, comparable to that of oxaliplatin (5 mg/kg, i.p.). The combined administration of rafoxanide and oxaliplatin produced a synergistic therapeutic effect. First to indicate that rafoxanide inhibits CDK4/6 activity and is a potential candidate drug for the treatment of human skin cancer[1].
Cell Research Cell cycle analysis using an EPICS XL4 Flow Cytometer.?The cell cycle phase distribution was analyzed using ModFit LT 2.0 software.?Briefly, cells (4x10^4 ) were seeded in 24-well plates in DMEM containing 0.125% FBS.?After 24 h, the cell culture medium was replaced with DMEM containing 10% FBS and various doses of rafoxanide (1, 3, 10 or 30 μM) for 6, 12 or 24 h, as indicated.?At the end of the experiments, cells (1x10^4 ) were fixed in ice cold 70% ethanol, and stained using a Coulter DNA Prep Reagent kit , and cellular DNA content was assessed.?All data were obtained from two separate experiments performed in triplicate[1]
Animal Research A375 cells (1x10^6 ) were suspended in 0.2 ml PBS, and injected subcutaneously into the right flank of the mice (n=3).?Tumor size was assessed using a caliper.?When the tumors grew to 80-100 mm^3 (1 week after inoculation), mice were divided randomly into different experimental groups (5 mice/group), and intraperitoneally injected daily for 21 days with various testing compounds(Rafoxanide).?The mice were sacrificed by cervical dislocation, and the tumors were excised, weighed, and images were captured by camera .?The tumor volume was calculated using the formula V = ab^2 /2 (a = longest axis;?b = shortest axis)[1].
Molecular Weight 626.01
Formula C19H11Cl2I2NO3
CAS No. 22662-39-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL (49.52 mM)

TargetMolReferences and Literature

1. Shi X, Li H, Shi A et al.Discovery of rafoxanide as a dual CDK4/6 inhibitor for the treatment of skin cancer[J].Oncol Rep. 2018 Sep;40(3):1592-1600. 2. Xiao W , Xu Z , Chang S , et al. Rafoxanide, an organohalogen drug, triggers apoptosis and cell cycle arrest in multiple myeloma by enhancing DNA damage responses and suppressing the p38 MAPK pathway[J]. Cancer Letters, 2019, 444:45-59.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Parasitic Compound Library Inhibitor Library Kinase Inhibitor Library Anti-Prostate Cancer Compound Library FDA-Approved & Pharmacopeia Drug Library Cell Cycle Compound Library Anti-Breast Cancer Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Bioactive Compound Library

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FMF-04-159-2 Palbociclib BRD6989 Aloisine B Amsilarotene SNX7 CDK8/19-IN-1 BX-912

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Keywords

Rafoxanide 22662-39-1 Cell Cycle/Checkpoint Microbiology/Virology CDK Parasite Hemonchus energy metabolism inhibit antiparasitic Fasciola Estrus ovis halogenated salicylaniline uncoupling oxidative phosphorylation Inhibitor inhibitor

 

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