XS-060
Based on 1 Customer Validation
XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.67%
- No. CAS: 346721-50-4
- Fòrmula: C20H18N2O3
- Peso molecular:334.37
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
RXRα (Retinoid X receptor alpha)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>30 μM
Compound: S19
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Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs
Inhibition of IDO1 in IFN-gamma stimulated human HeLa cells assessed as reduction in kynurenine production using L-tryptophan as substrate incubated for 24 hrs
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[PMID: 31610376] |
| MDA-MB-231 | IC50 |
6.88 μM
Compound: XS-060
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Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
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[PMID: 37058970] |
XS-060 targeting the RXRα′ s coactivator binding site can inhibit pRXRα-PLK1 interaction and exhibits good antitumor activity as an anti-mitotic agent[1].
XS-060 shows anti-proliferative activity against MDA-MB 231 cancer cells, with an IC50 of 6.880 ± 0.059 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB 231, A549, and HepG2
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Concentration:5 μM
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Incubation Time:
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Result:Showed anti-proliferative activity at 5 μM against cancer cells (MDA-MB 231, A549, and HepG2), with cell viability rate (%) of 51.93 ± 4.32, 82.65 ± 2.84, and 48.65 ± 6.45, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (10-14 weeks, 200-220g)[1]
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Dosage:25 mg/kg
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Administration:Oral absorption (p.o.) and intraperitoneal injection (i.p.), once, (Pharmacokinetic Analysis)
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Result:The oral absorption of XS-060 is very poor, while intraperitoneal injection displayed good absorption[1].
Pharmacokinetic Parameters of XS-060 in Sprague-Dawley rats[1].
XS060 25 mg/kg (i.p.) Tmax (h) 2.67 ± 1.12 Cmax (μg/L) 1061.50 ± 399.20 AUC0-∞ (μg⋅h/L) 7040.30 ± 1593.52 T1/2 (h) 2.13 ± 0.05 CLz/F (L/(h⋅kg)) 3.67 ± 0.81 Vd, z/F (L/kg) 11.31 ± 2.71