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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

View related series

Androgen receptor Antagonist

Basic Description

Synonyms	apalutamide\|ARN-509\|956104-40-8\|Erleada\|JNJ-56021927\|ARN 509\|Apalutamide [INN]\|ARN509\|UNII-4T36H88UA7\|4T36H88UA7\|Apalutamide (ARN-509)\|4-(7-(6-CYANO-5-(TRIFLUOROMETHYL)PYRIDIN-3-YL)-8-OXO-6-THIOXO-5,7-DIAZASPIRO[3.4]OCTAN-5-YL)-2-FLUORO-N-METHYLBENZAMIDE\|
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

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Discover Target: CYP3A4

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

GABRA1 Tclin Gamma-aminobutyric acid receptor subunit alpha-1 0 Activities

Discover Target: GABRA1

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

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

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

AR Tclin Androgen receptor 5 Activities

Discover Target: AR

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

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

Certificates

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1 results found

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]
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]
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]

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