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Tamibarotene Retinoid Receptor agonist

Name: Tamibarotene
SKU: S4260
Availability: InStock
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Cat.No.S4260

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

Chemical Structure

Molecular Weight: 351.44

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
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Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	351.44	Formula	C₂₂H₂₅NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	94497-51-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Am 80			Smiles	CC1(CCC(C2=C1C=CC(=C2)NC(=O)C3=CC=C(C=C3)C(=O)O)(C)C)C

Solubility

In vitro
Batch:

DMSO : 70 mg/mL (199.18 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 70 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.500mg/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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.150mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.500mg/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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.550mg/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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	RARα ^[1] RARβ ^[1]
In vitro	Tamibarotene slightly inhibits the growth of both myeloma cells and HUVECs, and remarkably inhibits the growth of HUVECs stimulated by VEGF. This compound shows little growth inhibition of bone marrow stromal cells (BMSCs), but it markedly inhibits migration of HUVECs by cocultured myeloma cells. It inhibits VEGF-induced phosphorylation of VEGF receptor. The compound significantly inhibits VEGF-induced formation of tube-like structures in vitro and neovascularization in mouse corneas. ^[1] This chemical-induced HL-60 cell adhesion to ECs is 38% lower than All-trans retinoic acid (ATRA), and NB4 cell adhesion to ECs by this compound 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. It induces only the early-phase induction in HL-60 cells, resulting in its lower CD38 induction than ATRA. ^[2] This agent has negligible growth inhibition of peripheral blood mononuclear cells but marked growth inhibition of both HTLV-I-infected T-cell lines and ATL cells. It arrests cells in the G1 phase of the cell cycle and induces apoptosis in HTLV-I-infected T-cell lines. The compound 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. It also inhibits the expression of JunD, resulting in suppression of AP-1-DNA binding. ^[3]
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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/15843826/ [2] https://pubmed.ncbi.nlm.nih.gov/21393419/ [3] https://pubmed.ncbi.nlm.nih.gov/18771528/ [4] https://pubmed.ncbi.nlm.nih.gov/19571405/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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