AM-80

SKU: orb1300549

Description

Tamibarotene is a synthetic oral retinoid developed to target ATRA-resistant cancers. It exhibits antineoplastic activity and is utilized in oncology research, particularly for acute promyelocytic leukemia (APL), with studies conducted in both cellular and animal models.

Research Area

Immunology & Inflammation, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 94497-51-5
• MW: 351.4
• Purity: >98%
• Formula: C₂₂H₂₅NO₃
• SMILES: CC1(C)C=2C(=CC(NC(=O)C3=CC=C(C(O)=O)C=C3)=CC2)C(C)(C)CC1
• Target: Retinoid receptor and related
• Solubility: Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 18 mg/ml).

Bioactivity

• In Vivo:
  Tamibarotene induced HL-60 cell adhesion to endothelial cells was 38% lower compared to all-trans retinoic acid (ATRA). However, its ability to induce NB4 cell adhesion to endothelial cells was comparable to ATRA. In HL-60 cells, tamibarotene uniquely promoted early-phase induction of CD38 gene transcription through DR-RARE with intron 1 and late-phase induction through RARE lacking a 5' flanking region, resulting in lower CD38 induction than ATRA. Tamibarotene's growth inhibition on peripheral blood mononuclear cells was negligible, but it significantly inhibited growth in HTLV-I infected T-cell lines and ATL cell markers. It induced G1 phase cell cycle arrest and apoptosis in HTLV-I infected T-cell lines, inhibited phosphorylation of IkappaBalpha and NF-κB-DNA binding, reduced expression of proteins involved in G1/S phase cell cycle transition and apoptosis, and suppressed JunD expression, inhibiting AP-1 DNA binding. Tamibarotene slightly inhibited the growth of myeloma cells and HUVECs, and significantly inhibited VEGF-stimulated HUVEC growth. While having minimal growth inhibition on bone marrow stromal cells (BMSC), tamibarotene significantly inhibited HUVEC migration when co-cultured with myeloma cells and inhibited VEGF-induced phosphorylation of the VEGF receptor. Tamibarotene markedly suppressed the formation of in vitro tubular structures and neovascularization induced by VEGF in mouse cornea.
• In Vitro:
  Tamibarotene treatment significantly reduces the levels of insoluble amyloid beta (Aβ) in the mice's brain, particularly Aβ(42), without notably affecting the levels of soluble Aβ.
• Cell Research:
  The CellTiter Aqueous Non-Radioactive Cell Proliferation Assay Kit is used to assess cell growth. Briefly, 10,000 cells per well are seeded in a 96-well plate and cultured in RPMI containing 2% charcoal-stripped FBS and indicated retinoid concentrations for 72 hours. At the end of the treatment period, the MTS reagent is added, cells are incubated an additional 2-4 hours, and absorbance is measured at 490 nanometers.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tamibarotene; NSC608000; Retinobenzoic acid

Compound Identifiers

PubChem CID

108143