PA 452

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Cat.No. 5086 - PA 452 | C26H37N3O3 | CAS No. 457657-34-0
Description: RXR antagonist
Chemical Name: 2-[[3-(Hexyloxy)-5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl]methylamino]-5-pyrimidinecarboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

RXR antagonist (pA2 = 7.11). Triggers dissociation of RXR tetramers. Attenuates cell proliferation and induces apoptosis in MCF-7 breast cancer cells.

Compound Libraries

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Technical Data

M. Wt 439.59
Formula C26H37N3O3
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 457657-34-0
PubChem ID 9803242
InChI Key JJUUTJCZMGZJDZ-UHFFFAOYSA-N
Smiles CC1(C)C2=C(C=C(N(C3=NC=C(C(O)=O)C=N3)C)C(OCCCCCC)=C2)C(C)(C)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.96 100
ethanol 4.4 10

Preparing Stock Solutions

The following data is based on the product molecular weight 439.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.27 mL 11.37 mL 22.75 mL
5 mM 0.45 mL 2.27 mL 4.55 mL
10 mM 0.23 mL 1.14 mL 2.27 mL
50 mM 0.05 mL 0.23 mL 0.45 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Yasmin et al (2010) Inhibition of mammary carcinoma cell growth by RXR is mediated by the receptor's oligomeric switch. J.Mol.Biol. 397 1121 PMID: 20188110

Takahashi et al (2002) Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions. J.Med.Chem. 45 3327 PMID: 12139443

Nakayama et al (2011) Discovery of a potent retinoid X receptor antagonist structurally closely related to RXR agonist NEt-3IBIB. J.Med.Chem.Lett 2 896 PMID: 24900278


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Keywords: PA452 RXR tetramers retinoid X receptors antagonists Retinoid X Receptor

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Literature in this Area

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Retinoid Receptors Scientific Review

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Pathways for PA 452

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