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ARN-509 - ≥98%, high purity , Androgen Receptor antagonist, CAS No.956104-40-8, Androgen Receptor antagonist

Moligand™

≥98%

CAS#: 956104-40-8
Formula: C₂₁H₁₅F₄N₅O₂S
Molecular Weight: 477.43
PubChem CID: 24872560

Item Number

A127949

Grouped product items
SKU	Size	Availability	Price
A127949-5mg	5mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$195.90
A127949-25mg	25mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$880.90
A127949-100mg	100mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$3,170.90

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Androgen receptor Antagonist

Basic Description

Synonyms	Uremide \| Erleada (TN) \| Z2037280438 \| Erleada \| HY-16060 \| 4-{7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl}-2-fluoro-N-methylbenzamide \| APALUTAMIDE [MI] \| SCHEMBL909297 \| CCG-264760 \| MFCD22380626 \| NCG
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that can
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Androgen Receptor antagonist
Note	卖完停产，不再备货
Product Description	ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment.

Associated Targets(Human)

AR Tclin Androgen receptor (5 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen Receptor (11781 Activities)

Discover Target: AR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)

Discover Target: CYP3A4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

LNCaP (8286 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)

Discover Target: Hdac6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mus musculus (284745 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Rattus norvegicus (775804 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 Activities)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Gabrp GABA-A receptor; anion channel (5731 Activities)

Discover Target: Gabrp

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Names and Identifiers

IUPAC Name	4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide
INCHI	InChI=1S/C21H15F4N5O2S/c1-27-17(31)13-4-3-11(8-15(13)22)30-19(33)29(18(32)20(30)5-2-6-20)12-7-14(21(23,24)25)16(9-26)28-10-12/h3-4,7-8,10H,2,5-6H2,1H3,(H,27,31)
InChi Key	HJBWBFZLDZWPHF-UHFFFAOYSA-N
Canonical SMILES	CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CC(=C(N=C4)C#N)C(F)(F)F)F
Isomeric SMILES	CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CC(=C(N=C4)C#N)C(F)(F)F)F
PubChem CID	24872560
Molecular Weight	477.43

PubChem CID

ChEMBL Ligand

CAS Registry No.

DrugCentral Ligand

Lot Number

Certificate Type

Date

Item

D1725131

Certificate of Analysis

Nov 16, 2022

A127949

Safety and Hazards(GHS)

Pictogram(s)	GHS08, GHS09, GHS07
Signal	Danger
Hazard Statements	H373:Causes damage to organs through prolonged or repeated exposure H302:Harmful if swallowed H410:Very toxic to aquatic life with long lasting effects H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H361:Suspected of damaging fertility or the unborn child
Precautionary Statements	P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P391:Collect spillage. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell.

References

1. Jung ME, Ouk S, Yoo D, Sawyers CL, Chen C, Tran C, Wongvipat J. (2010) Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).. J Med Chem, 53 (7): (2779-96). [PMID:20218717] [10.1021/op500134e]
2. Rathkopf DE, Morris MJ, Fox JJ, Danila DC, Slovin SF, Hager JH, Rix PJ, Chow Maneval E, Chen I, Gönen M et al.. (2013) Phase I study of ARN-509, a novel antiandrogen, in the treatment of castration-resistant prostate cancer.. J Clin Oncol, 31 (28): (3525-30). [PMID:24002508] [10.1021/op500134e]
3. Smith MR, Saad F, Chowdhury S, Oudard S, Hadaschik BA, Graff JN, Olmos D, Mainwaring PN, Lee JY, Uemura H et al.. (2018) Apalutamide Treatment and Metastasis-free Survival in Prostate Cancer.. N Engl J Med, 378 (15): (1408-1418). [PMID:29420164] [10.1021/op500134e]

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ARN-509 - ≥98%, high purity , Androgen Receptor antagonist, CAS No.956104-40-8, Androgen Receptor antagonist

Basic Description

Product Properties

Associated Targets(Human)

Associated Targets(non-human)

Mechanisms of Action

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

Chemical and Physical Properties

Safety and Hazards(GHS)

Related Documents

References

Solution Calculators

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