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Rafoxanide

SKU: orb1225602

Description

A salicylanilide anthelmintic agent that also shows to be an allosteric inhibitor of SPAK and OSR1; has antiangiogenic activity in zebrafish with IC50 of 1.69 uM on the intersegmental vessels and 1.45 uM on the subintestinal vessels.Parasite Infection Approved.

Images & Validation

Key Properties

CAS Number22662-39-1
MW626.0105
Purity>98% (HPLC)
FormulaC19H11Cl2I2NO3
SMILESC1=CC(=CC=C1OC2=C(C=C(C=C2)NC(=O)C3=C(C(=CC(=C3)I)I)O)Cl)Cl
TargetParasite
SolubilityDMSO: ≥ 31 mg/mL

Bioactivity

In Vivo
Animal model: AOM induced Apcmin/+mice. Dosage: 7.5 mg/kg. Administration: Intraperitoneal injection (i.p.), once every 2 d for 88d. Result: Exerted less number and size of AOM induced lesions in the colon. No significant body weight changes were observed. Detected adenomas (28.6%), advanced adenomas (67.8%) and adenocarcinoma (3.6%) in control group as adenomas (33.3%), advanced adenomas (25%%) and no obvious lesions(41.6%) were detected in treated group. Caused increased signal for p-eIF2α, CHOP and cleaved caspase-3 in tumor tissues while these signal in non-tumor colon epithelium were barely detectable.
In Vitro
Western blot analysis. Cell line: HCT-116. Concentration: 1.25, 2.5, 5 μM Incubation time: 24 h. Result: Increased phosphorylate eIF2α and CHOP, which is the hallmark feature of ERS. Apoptosis Analysis Cell line: HCEC-1CT, HCT-116 and DLD-1. Concentration: 1.25, 2.5, 5 μM Incubation time: 24, 48, 60 h. Result: Detected cell death of HCT-116 and DLD-1 from 48 h while no significant cell death was observed in HCEC-1CT. Pre-incubation of CRC cells with the pan-caspase inhibitor Q-VD-OPH totally reverted the rafoxanide-induced cell death, indicating the involvement of apoptotic pathways.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Rafoxanide | BRN 2228187 | Disalan | Duofas | EINECS 245-148-9

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Rafoxanide (orb1225602)

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