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Tazarotene Retinoid Receptor agonist

Cat.No.S1569

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

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 10 mg/mL (28.45 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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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Chemical Information, Storage & Stability

Molecular Weight 351.46 Formula

C21H21NO2S

Storage (From the date of receipt)
CAS No. 118292-40-3 Download SDF Storage of Stock Solutions

Synonyms AGN190168 SMILES CCOC(=O)C1=CN=C(C=C1)C#CC2=CC3=C(C=C2)SCCC3(C)C

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Mechanism of Action

Targets/IC50/Ki
RAR
In vitro
Tazarotene causes ERK activation, RB tumor suppressor protein hypophosphorylation, G0 arrest, and myeloid differentiation in HL-60 human myeloblastic leukemia cells. This compound could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective ligand. It regulates gene transcription via interaction with specific nuclear retinoic acid receptors (RARs), thereby modulating the three key pathogenic factors in psoriasis. This chemical inhibits the proliferation of fibroblasts and synthesis of DNA and collagen. It down-regulates markers of keratinocyte differentiation, keratinocyte proliferation, and inflammation. This agent also up-regulates three novel genes TIG-1 (tazarotene-induced gene-1), TIG-2, and TIG-3, which may mediate an antiproliferative effect. It causes growth suppression in retinoid-responsive breast cancer cell lines by up-regulating TIG3.
In vivo
Tazarotene treatment reduces the number and size of microscopic basal cell carcinomas (BCCs) in UV-treated Ptch1+/− mice. This compound also reduces the number and size of microscopic basal cell carcinomas (BCCs) in ionizing radiation-treated Ptch1+/− mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9270552/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15231643/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-30)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06331624 COMPLETED
Idiopathic Pulmonary Fibrosis; IPF
GRI Bio Operations, Inc.
2024-04-24 PHASE2
NCT06042647 COMPLETED
Psoriasis Vulgaris
Dermatology Consulting Services, PLLC
2023-07-13 PHASE4
NCT05872256 COMPLETED
Scalp Psoriasis
Dermatology Consulting Services, PLLC
2023-06-01 PHASE4
NCT05555797 UNKNOWN
Psoriasis
Assiut University
2022-10-30 PHASE4
NCT06015152 COMPLETED
Scalp Psoriasis
Jinnah Postgraduate Medical Centre
2022-08-01
NCT05314127 UNKNOWN
Warts Flat
Zagazig University
2022-04-15 PHASE2

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