AGN 195183

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation. Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients.

Product information

CAS Number: 191469-29-1

Molecular Weight: 387.42

Formula: C22H23F2NO3

Synonym:

AGN195183

AGN-195183

Chemical Name: 2,6-difluoro-4-(5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-amido)benzoic acid

Smiles: CC1(C)CCC(C)(C)C2=CC=C(C=C12)C(=O)NC1=CC(F)=C(C(O)=O)C(F)=C1

InChiKey: WTKJHVPWANEVRO-UHFFFAOYSA-N

InChi: InChI=1S/C22H23F2NO3/c1-21(2)7-8-22(3,4)15-9-12(5-6-14(15)21)19(26)25-13-10-16(23)18(20(27)28)17(24)11-13/h5-6,9-11H,7-8H2,1-4H3,(H,25,26)(H,27,28)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 11 mg/mL (25.12 mM; Need ultrasonic)

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

References:

1. Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.

Products are for research use only. Not for human use.