Rafoxanide

SKU: orb1300080

Description

Rafoxanide is a repurposed salicylanilide anthelmintic now identified as a dual CDK4/6 inhibitor. It demonstrates potential in skin cancer research, showing antitumor activity in both in vitro cellular assays and in vivo mouse models of melanoma.

Research Area

Cell Biology, Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 22662-39-1
• MW: 626.01
• Purity: >99.99% (May vary between batches)
• Formula: C₁₉H₁₁Cl₂I₂NO₃
• SMILES: OC1=C(C=C(I)C=C1I)C(=O)NC1=CC=C(OC2=CC=C(Cl)C=C2)C(Cl)=C1
• Target: Apoptosis,OXPHOS,Raf,p38 MAPK,CDK,Parasite
• Solubility: DMSO:6.27 mg/mL (10.02 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.6 mM)

Bioactivity

• 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.
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• 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.
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• 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
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Rafoxanide, uncoupling oxidative phosphorylation, CDK6, CDK4, antiparasitic, Fasciola, energy metabolism, halogenated salicylaniline, Estrus ovis, Inhibitor, Hemonchus, Parasite, inhibit

Compound Identifiers

PubChem CID

31475