Home Metabolism Retinoid Receptor agonist Tamibarotene For research use only.

Tamibarotene

Synonyms: Am 80

Tamibarotene(Am 80) is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ.

Tamibarotene Chemical Structure

Tamibarotene Chemical Structure

CAS: 94497-51-5

Selleck's Tamibarotene has been cited by 2 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
NB4 cells Proliferation assay 48 h Antiproliferative activity against human NB4 cells after 48 hrs by MTT assay, IC50=4.81 μM 22014829
HL60 cells Proliferation assay Antiproliferative activity against human HL60 cells, IC50=6 μM 19443225
HL60 cells Proliferation assay 48 h Antiproliferative activity against human HL60 cells after 48 hrs by MTT assay, IC50=8.94 μM 22014829
Jurkat cells Proliferation assay Antiproliferative activity against human Jurkat cells, IC50=17.3 μM 19443225
MOLT4 cells Proliferation assay Antiproliferative activity against human MOLT4 cells, IC50=19.5 μM 19443225
U937 cells Proliferation assay Antiproliferative activity against human U937 cells, IC50=20.2 μM 19443225
K562 cells Proliferation assay 48 h Antiproliferative activity against human K562 cells after 48 hrs by MTT assay, IC50=42.37 μM 22014829
COS-1 cells Function assay Transcriptional activation in COS-1 cells expressing Retinoic Acid Receptor alpha (RAR alpha) 10669568
Click to View More Cell Line Experimental Data

Biological Activity

Description Tamibarotene(Am 80) is a synthetic retinoic acid receptor (RAR) agonist with high specificity for RARα and RARβ over RARγ.
Targets
RARα [1] RARβ [1]
In vitro
In vitro

Tamibarotene slightly inhibits the growth of both myeloma cells and HUVECs, and remarkably inhibits the growth of HUVECs stimulated by VEGF. Tamibarotene shows little growth inhibition of bone marrow stromal cells (BMSCs), but it markedly inhibits migration of HUVECs by cocultured myeloma cells. Tamibarotene inhibits VEGF-induced phosphorylation of VEGF receptor. Tamibarotene significantly inhibits VEGF-induced formation of tube-like structures in vitro and neovascularization in mouse corneas. [1] Tamibarotene-induced HL-60 cell adhesion to ECs is 38% lower than All-trans retinoic acid (ATRA), and NB4 cell adhesion to ECs by tamibarotene is equivalent to ATRA, which induces CD38 gene transcription biphasically in HL-60 cells, the early-phase induction via DR-RARE containing intron 1, and the delayed-phase induction via RARE lacking the 5'-flanking region. Tamibarotene induces only the early-phase induction in HL-60 cells, resulting in its lower CD38 induction than ATRA. [2] Tamibarotene has negligible growth inhibition of peripheral blood mononuclear cells but marked growth inhibition of both HTLV-I-infected T-cell lines and ATL cells. Tamibarotene arrests cells in the G1 phase of the cell cycle and induces apoptosis in HTLV-I-infected T-cell lines. Tamibarotene inhibits also the phosphorylation of IkappaBalpha and NF-kappaB-DNA binding, in conjunction with reduction of expression of proteins involved in the G1/S cell cycle transition and apoptosis. Tamibarotene also inhibits the expression of JunD, resulting in suppression of AP-1-DNA binding. [3]
In Vivo
In vivo

Tamibarotene treatment reduces significantly the insoluble Abeta levels in brain of mice, in particular Abeta(42), while it gives no apparent effects on the soluble Abeta levels. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04905407 Recruiting Acute Myeloid Leukemia Syros Pharmaceuticals August 26 2021 Phase 2
NCT00985530 Terminated Acute Promyelocytic Leukemia Northwestern University|CytRx|Cephalon October 2009 Phase 1
NCT00520208 Completed Acute Promyelocytic Leukemia CytRx September 2007 Phase 2

Chemical lnformation & Solubility

Molecular Weight 351.44 Formula

C22H25NO3
CAS No. 94497-51-5 SDF Download Tamibarotene SDF
Smiles CC1(CCC(C2=C1C=CC(=C2)NC(=O)C3=CC=C(C=C3)C(=O)O)(C)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (199.18 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 70 mg/mL

Water : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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