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367273-07-2 (AGN 195183)

1

Identification

AGN 195183 AGN 195183
Name AGN 195183
Formula C22H22ClF2NO4
MW 437.86
CAS No. 367273-07-2
EINECS
Smiles O=C(O)C1=C(F)C=C(NC(C2=C(O)C(Cl)=C3C(C)(C)CCC(C)(C)C3=C2)=O)C=C1F
Synonyms AGN195183;AGN-195183; 4-(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-5,6,7,8-tetrahydronaphthalene-2-carboxamido)-2,6-difluorobenzoic acid
InChI InChI=1S/C22H22ClF2NO4/c1-21(2)5-6-22(3,4)16-12(21)9-11(18(27)17(16)23)19(28)26-10-7-13(24)15(20(29)30)14(25)8-10/h7-9,27H,5-6H2,1-4H3,(H,26,28)(H,29,30)
2

Introduction

AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.) Target: RARα agonist Compound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation. Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580.

Background Information

AGN 195183 is a potent and selective agonist of RARα (Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ. ......by AdooQ BioScience, LLC
RX-195183 is an RARα agonist (Kd=3 nM) with potential antineoplastic activity, modulating the transcription of genes responsible for cell differentiation and proliferation. ......by BOC Sciences
NRX-195183 is an orally bioavailable retinoid acid receptor (RAR) alpha agonist with potential antineoplastic activity. Retinoid analogue NRX 195183 binds to and activates RAR alpha, modulating the transcription of genes responsible for cell differentiation and proliferation, which may result in cell differentiation, decreased cell proliferation, and the inhibition of tumorigenesis. Encoded by the RARA gene, RAR alpha is a nuclear receptor and a member of the steroid receptor superfamily. ......by MedKoo Biosciences, Inc.
A potent, selective RARα agonist; significantly reduces albuminuria and normalizes blood pressure, lowers glomerulosclerosis index, glomerular cell and interstitial cell counts, and area of the interstitial space in nephritic rats; reduces renal damage in rats with established chronic glomerulonephritis. ......by ProbeChem
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000073803

Storage condition

Store in a tightly closed container, in a cool and dry place. by MedChemexpress Co., Ltd.

Solubility

10 mM in DMSO by CHEMSCENE, LLC
10 mM in DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

Signaling Pathways Metabolic Enzyme/Protease
Target RAR/RXR
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
AGN 195183 - Phase 2 Clinical
AGN 195183 - No Development Reported
7

Safety Data of AGN 195183

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC USA
Ark Pharm, Inc. USA
BOC Sciences
CHEMSCENE, LLC 5mg/USD420();10mg/USD600() USA
MedChemexpress Co., Ltd. 5mg/USD420();10mg/USD600() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD420();10mg/USD600() China
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Related Products

Other Forms of 367273-07-2

Name CAS No Formula MW

Recommended Compounds in RAR/RXR

Name CAS No Formula MW
AGN 205728 859498-05-8 C29H27NO3 437.53
AGN 196996 958295-17-5 C24H20BrNO5 482.32
AGN 194310 229961-45-9 C28H24O2S 424.55
Acitretin (sodium) 925701-88-8 C21H25NaO3 348.41
Acitretin 55079-83-9 C21H26O3 326.43
Adapalene (sodium salt) 911110-93-5 C28H27NaO3 434.5
Adapalene 106685-40-9 C28H28O3 412.52
TTNPB 71441-28-6 C24H28O2 348.48
Magnolol 528-43-8 C18H18O2 266.33
Tazarotene 118292-40-3 C21H21NO2S 351.46
Fenretinide 65646-68-6 C26H33NO2 391.55
LG 100268 153559-76-3 C24H29NO2 363.49
Isotretinoin 4759-48-2 C20H28O2 300.44
Palovarotene 410528-02-8 C27H30N2O2 414.54
Retinoic acid 302-79-4 C20H28O2 300.44
AM580 102121-60-8 C22H25NO3 351.44
(R)-Flurbiprofen 51543-40-9 C15H13FO2 244.2609
Tamibarotene 94497-51-5 C22H25NO3 351.44
Bexarotene 153559-49-0 C24H28O2 348.48
AR7 80306-38-3 C15H12ClNO 0.0

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

AGN 195183

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