Tazarotene

Synonyms: AGN190168

Tazarotene (AGN190168) is a retinoid prodrug of tazarotenic acid, which is a RAR agonist, used to treat psoriasis, acne, and sun damaged skin.

Tazarotene  Chemical Structure

Tazarotene Chemical Structure

CAS: 118292-40-3

Selleck's Tazarotene has been cited by 3 publications

Purity & Quality Control

Batch: Purity: 99.98%
99.98

Choose Selective Retinoid Receptor Inhibitors

Biological Activity

Description Tazarotene (AGN190168) is a retinoid prodrug of tazarotenic acid, which is a RAR agonist, used to treat psoriasis, acne, and sun damaged skin.
Targets
RAR [1]
In vitro
In vitro Tazarotene causes ERK activation, RB tumor suppressor protein hypophosphorylation, G0 arrest, and myeloid differentiation in HL-60 human myeloblastic leukemia cells. Tazarotene could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective ligand. [1] Tazarotene therapy regulates gene transcription via interaction with specific nuclear retinoic acid receptors (RARs), thereby modulating the three key pathogenic factors in psoriasis. [2] Tazarotene inhibits the proliferation of fibroblasts and synthesis of DNA and collagen. [3] Tazarotene down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation. Tazarotene also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect. [4] Tazarotene causes growth suppression in retinoid-responsive breast cancer cell lines by up-regulating TIG3. [5]
In Vivo
In vivo Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in UV-treated Ptch1+/− mice. Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in ionizing radiation-treated Ptch1+/− mice. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06015152 Completed Scalp Psoriasis Jinnah Postgraduate Medical Centre August 1 2022 Not Applicable
NCT03988439 Recruiting Psoriasis Bausch Health Americas Inc. March 24 2021 Phase 4
NCT02620813 Completed Acne Vulgaris University of California Davis October 2015 Early Phase 1

Chemical lnformation & Solubility

Molecular Weight 351.46 Formula

C21H21NO2S

CAS No. 118292-40-3 SDF Download Tazarotene SDF
Smiles CCOC(=O)C1=CN=C(C=C1)C#CC2=CC3=C(C=C2)SCCC3(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 10 mg/mL ( (28.45 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble


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In vivo
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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.

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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

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