1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. RAR/RXR
  3. XS-060

XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction.

For research use only. We do not sell to patients.

XS-060 Chemical Structure

XS-060 Chemical Structure

CAS No. : 2787626-06-4

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Description

XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction[1].

IC50 & Target

RXRα (Retinoid X receptor alpha)[1]

In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: MDA-MB 231, A549, and HepG2
Concentration: 5 μM
Incubation Time:
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.
In Vivo

XS-060 (25 mg/kg, IP or PO, once) displays good absorption by intraperitoneal injection, but oral absorption is very poor[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley rats (10-14 weeks, 200-220g)[1]
Dosage: 25 mg/kg
Administration: Oral absorption (p.o.) and intraperitoneal injection (i.p.), once, (Pharmacokinetic Analysis)
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
Molecular Weight

334.37

Formula

C20H18N2O3

CAS No.
SMILES

COC(C=C1)=CC=C1CC(N/N=C/C2=C(O)C=CC3=C2C=CC=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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XS-060
Cat. No.:
HY-149085
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