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WYC-209

SKU: orb1301872

Description

WYC-209 is a retinoic acid receptor (RAR)-targeting small molecule that potently suppresses the proliferation of malignant murine melanoma tumor-repopulating cells (TRCs) with an IC50 of 0.19 µM. This inhibitor is a useful research tool for studying RAR signaling in cancer stemness and tumorigenesis in both in vitro and in vivo models.

Research Area

Cell Biology, Metabolism Research

Images & Validation

Key Properties

CAS Number2131803-90-0
MW368.45
Purity98.91% (May vary between batches)
FormulaC20H20N2O3S
SMILESCCOC(=O)c1cnc(nc1)C#Cc1ccc2c(c1)C(C)(C)CCS2=O
TargetAutophagy,Retinoid Receptor,Apoptosis
SolubilityH2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (8.96 mM);DMSO:80 mg/mL (217.13 mM)

Bioactivity

Target IC50
TRC:0.19 μM
In Vivo
WYC-209 abrogates 87.5% of lung metastases of melanoma TRCs in immune-competent wild-type C57BL/6 mice at 0.22 mg kg-1 without showing apparent toxicity.
In Vitro
WYC-209 inhibits proliferation of malignant murine melanoma tumor-repopulating cells (TRCs), with an IC50 of 0.19 μM in a dose-dependent manner. WYC-209 also inhibits proliferation of TRCs of human melanoma, lung cancer, ovarian cancer, and breast cancer in culture.
Cell Research
Cell proliferation rate was measured by using MTT colorimetric assay. Cells were seeded in 3D soft fibrin gel in 96-well microplates at a density to maintain control (untreated) cells in an exponential phase of growth during the entire experiment. Cells were incubated with various concentrations of compounds for each time point followed by incubation with 50 μL MTT reagent for 3 h at 37 °C. After incubation, 150 μL MTT solvent was added and absorbance was measured at 570 nm. All experiments were repeated at least three times. The percentage of viable cells was calculated and averaged for each well: percent growth = (OD-treated cells/OD control cells) × 100, cell proliferation at each time point is normalized to base line cell survival at the time of initial compound treatment (day 0).
Animal Research
Four- to six-week-old female and male C57BL/6 mice were used in mice experiment. Mice were randomized into different groups. In metastasis experiment, B16-F1 cell spheroids were selected from 3D 90-Pa fibrin gels and pipetted to single cells. These TRCs were harvested and the cell number was counted under microscopy. The cells were then suspended in PBS with appropriate cell density. Thirty thousand TRCs were intravenously injected into the tail vein of each wild-type C57BL/6 mouse. Five days later, inoculated mice were intravenous implanted with 0.022 mg/kg WYC-209, 0.22 mg/kg WYC-209, or 0.1% DMSO every two days. The mice were euthanized and examined for lung tumor formation at day 30. In treated TRCs injected in vivo experiments, B16-F1 cells were seeded into 3D 90-Pa fibrin gels and treated with 10 μM WYC-209 or 0.1% DMSO on day 3, then isolated treated TRCs colonies on day 5 and pipetted into single cell. 30,000 of TRCs were intravenously injected into the tail vein of each wild-type C57BL/6 mouse. No blinding was performed in the mice experiments.

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Autophagy, Apoptosis, Inhibitor, inhibit, Retinoic acid receptors, RetinoidReceptor, Retinoid X receptors, Retinoid Receptor, RAR/RXR, RAR, WYC 209, WYC209, WYC-209

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  • WYC209 [orb1221041]

    >98% (HPLC)

    2131803-90-0

    368.45

    C20H20N2O3S

    5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 g, 500 mg, 200 mg
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Key Properties

No computed properties available.

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Protocol Information

WYC-209 (orb1301872)

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5 mg
¥ 1,300.00
10 mg
¥ 1,690.00
25 mg
¥ 2,990.00
50 mg
¥ 4,420.00
100 mg
¥ 6,890.00
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