Tamibarotene , ≥98% , 94497-51-5

Synonym(s):
AM80;Amnoid;AMNOLAKE;N-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl)-2-naphthyl)terephthalamic acid;N-(5,6,7,8-Tetrahydro-5,5,8,8-tetramethyl-2-naphthyl)terephthalamic acid

CAS NO.：94497-51-5

Empirical Formula: C22H25NO3

Molecular Weight: 351.44

MDL number: MFCD00866188

EINECS: 1806241-263-5

PRODUCT Properties

• Melting point: 231-232°C
• Boiling point: 449.6±45.0 °C(Predicted)
• Density: 1.154±0.06 g/cm3(Predicted)
• RTECS: DH6940000
• storage temp.: room temp
• solubility: Soluble to 50 mM in DMSO
• form: powder
• pka: 3.83±0.10(Predicted)
• color: white to off-white

Description and Uses

AM80 is a retinoic acid receptor agonist that is selective for RARα (K_d = 62 nM; AC₅₀ = 1.46 nM) compared to RARβ (K_d = 280 nM; AC₅₀ = 6.87 nM) and RARγ (K_d = 816 nM; AC₅₀ = 148.7 nM). It demonstrates greater specific binding to RARα compared to retinoic acid , which exhibits little selectivity across RARα, β, or γ. AM80 exhibits antiproliferative effects against acute promyelocytic leukemia cells, inducing human promyelocytic leukemia HL-60 cell differentiation with an ED₅₀ value of 0.79 nM. It has also been shown to suppress the growth of other myeloid and lymphoid malignant cells.

Tamibarotene, a retinoic acid receptor-α(RARα) agonist, was approved for the treatment of relapsed or refractory acute promyelocytic leukemia (APL) in Japan on June, 2005 and is currently marketed by Nippon Shinyaku Co. This novel drug has shown high remission rate among patients who have recurrent disease after all trans retinoic acid therapy.

Safety

• WGK Germany: 3