BMS 195614

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Cat.No. 3660 - BMS 195614 | C29H24N2O3 | CAS No. 253310-42-8
Description: Selective RARα antagonist
Alternative Names: BMS614
Chemical Name: 4-[[[5,6-Dihydro-5,5-dimethyl-8-(3-quinolinyl)-2-naphthalenyl]carbonyl]amino]benzoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Literature

Biological Activity

Neutral retinoic acid receptor (RAR) α-selective antagonist (Ki = 2.5 nM). Displays no significant effect on nuclear receptor corepressor (NCoR) binding; moderately decreases SMRT binding to RAR. Antagonizes agonist-induced coactivator (CoA) recruitment.

Technical Data

M. Wt 448.51
Formula C29H24N2O3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 253310-42-8
PubChem ID 445091
InChI Key WGLMBRZXZDAQHP-UHFFFAOYSA-N
Smiles O=C(NC4=CC=C(C(O)=O)C=C4)C3=CC1=C(C=C3)C(C)(C)CC=C1C2=CN=C(C=CC=C5)C5=C2

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 11.21 25

Preparing Stock Solutions

The following data is based on the product molecular weight 448.51. 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 2.23 mL 11.15 mL 22.3 mL
5 mM 0.45 mL 2.23 mL 4.46 mL
10 mM 0.22 mL 1.11 mL 2.23 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Gehin et al (1999) Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem.Biol. 6 519 PMID: 10421757

Germain et al (2009) Differential action on coregulator interaction defines retinoid agonists and neutral antagonists. Chem.Biol. 16 479 PMID: 19477412

Schoenermark et al (1999) Retinoid-mediated suppression of tumor invasion and matrix metalloproteinase synthesis. Ann.N.Y.Acad.Sci. 30 878 PMID:


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Keywords: BMS195614 retinoic acid receptor RAR alpha α RARa antagonists neutral selective BMS614 BMS614 Retinoic Acid Receptors

2 Citations for BMS 195614

Citations are publications that use Tocris products. Selected citations for BMS 195614 include:

Flamini et al (2014) Retinoic acid reduces migration of human breast cancer cells: role of retinoic acid receptor beta. J Cell Mol Med 18 1113 PMID: 24720764

Johansson et al (2013) Retinoic acid receptor alpha is associated with tamoxifen resistance in breast cancer. Nat Commun 4 2175 PMID: 23868472


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Pathways for BMS 195614

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