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Tamibarotene

Name: Tamibarotene
Brand: Selleck Chemicals
SKU: S4260
Rating: 5 (4 reviews)

Synonyms: Am 80

Catalog No.S4260 Purity:99.99%

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

Tamibarotene Chemical Structure

CAS No. 94497-51-5

Purity & Quality Control

Batch: Purity: 99.99%

99.99

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Cell Data

Cell Lines	Assay Type	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04905407	Recruiting	Acute Myeloid Leukemia	Syros Pharmaceuticals	August 26 2021	Phase 2
NCT02807558	Completed	Acute Myeloid Leukemia\|Myelodysplastic Syndrome	Syros Pharmaceuticals	September 20 2016	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

References

[4] Kawahara K, et al. Biol Pharm Bull, 2009, 32(7), 1307-1309.

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
	Clear solution	5% DMSO 1 95% Corn oil	1.15mg/ml (3.27mM)	Taking the 1 mL working solution as an example, add 50 μL of 23 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.5mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.5mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.55mg/ml (1.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 11 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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
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