2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. 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. 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.

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

XS-060 Chemical Structure

XS-060 Chemical Structure

CAS No. : 346721-50-4

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Based on 1 publication(s) in Google Scholar

XS-060 Related Antibodies

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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. 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[1][2].

IC50 & Target

RXRα (Retinoid X receptor alpha)[1]
Cellular Effect
Cell Line Type Value Description References
HeLa IC50
> 30 μM
Compound: S19
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
[PMID: 31610376]
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.

XS-060 Related Antibodies

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.
Appearance

Solid

Color

Off-white to yellow

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 175 mg/mL (523.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9907 mL 14.9535 mL 29.9070 mL
5 mM 0.5981 mL 2.9907 mL 5.9814 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9907 mL 14.9535 mL 29.9070 mL 74.7675 mL
5 mM 0.5981 mL 2.9907 mL 5.9814 mL 14.9535 mL
10 mM 0.2991 mL 1.4953 mL 2.9907 mL 7.4767 mL
15 mM 0.1994 mL 0.9969 mL 1.9938 mL 4.9845 mL
20 mM 0.1495 mL 0.7477 mL 1.4953 mL 3.7384 mL
25 mM 0.1196 mL 0.5981 mL 1.1963 mL 2.9907 mL
30 mM 0.0997 mL 0.4984 mL 0.9969 mL 2.4922 mL
40 mM 0.0748 mL 0.3738 mL 0.7477 mL 1.8692 mL
50 mM 0.0598 mL 0.2991 mL 0.5981 mL 1.4953 mL
60 mM 0.0498 mL 0.2492 mL 0.4984 mL 1.2461 mL
80 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.9346 mL
100 mM 0.0299 mL 0.1495 mL 0.2991 mL 0.7477 mL
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XS-060 Related Classifications

Help & FAQs
  • 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.

Keywords:

XS-060346721-50-4 XS060XS 060RAR/RXRRetinoic acid receptorsRetinoid X receptorsMDA-MB 231A549HepG2antitumoranti-mitoticpRXRα-PLK1 interactionInhibitorinhibitorinhibit

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