AGN-195183 - 99%, high purity , Retinoic acid receptor alpha agonist, CAS No.367273-07-2, Retinoic acid receptor alpha agonist

  • ≥99%
Item Number
A651924
Grouped product items
SKUSizeAvailabilityPrice Qty
A651924-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$300.90
A651924-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$450.90
A651924-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$900.90
A651924-50mg
50mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,350.90

Basic Description

SynonymsHY-16684 | 4-[(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalene-2-carbonyl)amino]-2,6-difluorobenzoic acid | RC87L028HU | SCHEMBL5531052 | VTP-5183 | Q27288046 | AGN 195183 | BDBM50120065 | DB05653 | CS-3203 | 4-[(4-Chloro-3-hydroxy-5,5,8,8-t
Specifications & Purity≥99%
Biochemical and Physiological MechanismsAGN-195183 (IRX-5183) is a potent and selective agonist of RARα ( K d =3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Action TypeAGONIST
Mechanism of actionRetinoic acid receptor alpha agonist
Product Description

AGN-195183 (IRX-5183) is a potent and selective agonist of RARα ( K d =3 nM) with improved binding selectivity relative to AGN 193836. AGN-195183 has no activity on RARβ/γ.

In Vitro

AGN-195183 (IRX-5183; Compound 4) inhibits the growth of breast cancer cell lines, and is inactive in an in vivo model of topical irritation.\nAGN-195183 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3. AGN-195183 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. AGN-195183 is currently in Phase I/IIA clinical trials in cancer patients. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:IC50 value: 3 nM (Kd),200 nM (EC80, RAR Trans)

Product Properties

ALogP6.4

Associated Targets(Human)

RARA Tclin Retinoic acid receptor alpha (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
RARA Tclin Retinoic acid receptor alpha (1324 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RARG Tclin Retinoic acid receptor gamma (1154 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RARB Tclin Retinoic acid receptor beta (1232 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SK-BR-3 (5175 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
T47D (39041 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
COS-7 (515 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 4-[(4-chloro-3-hydroxy-5,5,8,8-tetramethyl-6,7-dihydronaphthalene-2-carbonyl)amino]-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)
InChi Key PNAWUIKCVQSLFG-UHFFFAOYSA-N
Canonical SMILES CC1(CCC(C2=C1C=C(C(=C2Cl)O)C(=O)NC3=CC(=C(C(=C3)F)C(=O)O)F)(C)C)C
Isomeric SMILES CC1(CCC(C2=C1C=C(C(=C2Cl)O)C(=O)NC3=CC(=C(C(=C3)F)C(=O)O)F)(C)C)C
Alternate CAS 367273-07-2
PubChem CID 9867758
MeSH Entry Terms AGN 195183;AGN195183
Molecular Weight 437.86

Certificates

Certificate of Analysis(COA)

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Chemical and Physical Properties

SolubilityDMSO : 11 mg/mL (25.12 mM; Need ultrasonic)

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