BMS 195614 is a selective RARα antagonist . It can bind to the RARα subunit . BMS195614,4[[[[5,6-Dihydro-5,5-dimethyl-8-(3-quinolinyl)]-2-naphthalenyl] carbonyl]amino]benzoic acid , was considered to be retinoid antagonists as it inhibited all-transretinoic acid-induced (ATRA-induced) retinoic acid response elements-chloramphenicol acetyltransferase (RARE-CAT) reporter expression via concomitantly transfected retinoic acid receptors (RARs) . Retinoic acids (RAs) are the most notably biologically active derivatives (collectively referred to as retinoids) of vitamin A (retinol). Retinoic acids exert a wide variety of profound effects on cellular differentiation, vertebrate development and homeostasis . BMS 195614 reversed the induction effect of selective RARα agonists, AM580, AM80 and BMS 194753 on differentiation of the acute promyelocytic leukemia cell lines, NB4 and HL60 . Treatment with retinoic acid (RA) (10-6 M) for 72 hrs significantly reduced T47D breast cancer cells migration. But RA in combination with BMS 195614 did not affect the cell movement . In cells of a bovine stromal-vascular fraction from intramuscular fat, BMS 195614 significantly diminished the anti-adipogenic effect of ATRA . BMS 195614 displayed poor in vivo activity in mice when administered orally. Treatment with BMS 195614 at oral doses for 1 month showed no inhibition to spermatogenesis . Oral administration of BMS 195614 did not suppress spermatogenesis in mice .

Product information

CAS Number: 253310-42-8

Molecular Weight: 448.51

Formula: C29H24N2O3

Chemical Name: 4-[5,5-dimethyl-8-(quinolin-3-yl)-5,6-dihydronaphthalene-2-amido]benzoic acid

Smiles: CC1(C)CC=C(C2C=C(C=CC1=2)C(=O)NC1C=CC(=CC=1)C(O)=O)C1C=NC2=CC=CC=C2C=1

InChiKey: WGLMBRZXZDAQHP-UHFFFAOYSA-N

InChi: InChI=1S/C29H24N2O3/c1-29(2)14-13-23(21-15-19-5-3-4-6-26(19)30-17-21)24-16-20(9-12-25(24)29)27(32)31-22-10-7-18(8-11-22)28(33)34/h3-13,15-17H,14H2,1-2H3,(H,31,32)(H,33,34)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

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