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

Tamibarotene Related Products

Choose Selective Retinoid Receptor Inhibitors

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 Information & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Tamibarotene | Tamibarotene ic50 | Tamibarotene price | Tamibarotene cost | Tamibarotene solubility dmso | Tamibarotene purchase | Tamibarotene manufacturer | Tamibarotene research buy | Tamibarotene order | Tamibarotene mouse | Tamibarotene chemical structure | Tamibarotene mw | Tamibarotene molecular weight | Tamibarotene datasheet | Tamibarotene supplier | Tamibarotene in vitro | Tamibarotene cell line | Tamibarotene concentration | Tamibarotene nmr