• Search chemicals, activators, Inhibitors, APIs, intermediates and raw materials.

956104-40-8 (ARN-509)

1

Identification

ARN-509 ARN-509
Name ARN-509
Formula C21H15F4N5O2S
MW 477.43
CAS No. 956104-40-8
EINECS
Smiles O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F
Synonyms ARN 509; ARN509; 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
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)
2

Introduction

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. IC50 value: 16 nM Target: androgen receptor ARN-509 is an androgen receptor antagonist with potential antineoplastic activity.

Background Information

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. IC50 value: 16 nM Target: androgen receptor 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 cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. ......by MedChemexpress Co., Ltd.
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 cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) Shelf life: >2 years if stored properly Drug formulation: This drug may be formulated in DMSO ......by MedKoo Biosciences, Inc.
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. Phase 3. ......by Selleck Chemicals LLC
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. Phase 3. ......by Target Molecule Corp.
3

Protocol(Only for Reference)

Cell Experiment

Cell lines LNCaP/AR prostate cancer cell line
Conditions 10 μM; 48 hours
Method Cells are incubated for 48 hours, after which ARN-509 is added in a 16 μL volume to the RPMI culture medium. For the antagonist mode assay, the ARN-509 is diluted in culture medium also containing 30 pM R1881. After 7 days' incubation, 16 μL of CellTiter-Glo Luminescent Cell Viability Assay is added and Relative Luminescence Units (RLUs) measured.
Source Selleck Chemicals LLC

Animal Experiment

Animal Models Castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors
Dosage 30 mg/kg/day
Formulation 15% Vitamin E-TPGS and 65% of a 0.5% w/v CMC solution in 20 mM citrate buffer (pH 4.0)
Administration Orally
Source Selleck Chemicals LLC
4

Physical and Chemical Properties

Appearance:White to off-white solid EBNumber:EB000018876

Storage condition

Storage condition:Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). Stock solution storage:0 - 4 C for short term (days to weeks), or -20 C for long term (months). Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. by MedKoo Biosciences, Inc.

Solubility

DMSO 15 mg/mL Ethanol 5 mg/mL by MedChemexpress Co., Ltd.
Soluble in DMSO, not in water by MedKoo Biosciences, Inc.
(25°C) * In vitro DMSO 18 mg/mL (37.7 mM); Ethanol5 mg/mL (10.47 mM); Water<1 mg/mL (<1 mM); In vivo 0.5% CMC, pH4.014 mg/mL by Selleck Chemicals LLC
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
ARN-509 Aragon Pharmaceuticals Inc Hormone refractory prostate cancer 2013/10/31 2016/12/31 Phase 3 Clinical
ARN-509 Aragon Pharmaceuticals Inc Hormone dependent prostate cancer 2013/2/28 2018/2/28 Phase 2 Clinical
ARN-509 Aragon Pharmaceuticals Inc Hormone refractory prostate cancer 2010/7/31 2013/6/30 Phase 2 Clinical
ARN-509 Aragon Pharmaceuticals Inc 2013/3/31 2013/6/30 Phase 1 Clinical
ARN-509 Aragon Pharmaceuticals Inc; Johnson & Johnson Hormone refractory prostate cancer 2013/2/28 2014/2/1 Phase 1 Clinical
ARN-509 - Phase 3
7

Safety Data of ARN-509

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 10mg/USD150(In stock) USA
Apexbio Technology LLC 5mg/USD108(In stock) USA
BioVision, Inc., 5mg/USD115() USA
CHEMSCENE, LLC USA
Cayman Chemical Company 1mg/USD35() USA
MedChemexpress Co., Ltd. 5mg/USD70(In stock);10mg/USD120(In stock);50mg/USD350(In stock);100mg/USD550(In stock) USA
MedKoo Biosciences, Inc. 10mg/USD150() USA
Selleck Chemicals LLC 5mg/USD210(In stock);10mg/USD270(In stock);10mM/1mLIn DMSO/USD400(In stock);10mM(in 1mL DMSO)/USD504(in 1mL DMSO);50mg/USD970(In stock);100mg/USD1270(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD80(In stock);10mg/USD140(In stock);50mg/USD350(In stock);100mg/USD550(In stock) China
Target Molecule Corp. 10mg/USD124();50mg/USD339() USA
10

Related Products

Other Forms of 956104-40-8

Name CAS No Formula MW

Recommended Compounds in Androgen Receptor

Name CAS No Formula MW
Lupeol 545-47-1 C30H50O 426.72
Oxandrolone 53-39-4 C19H30O3 306.44
Testosterone undecylate 5949-44-0 C30H48O3 456.7
Spironolactone 52-01-7 C24H32O4S 416.57
LGD-4033 1165910-22-4 C14H12F6N2O 338.25
Adrenosterone 382-45-6 C19H24O3 300.39
Triptophenolide 74285-86-2 C20H24O3 312.4
Epiandrosterone 481-29-8 C19H30O2 290.44
3,3'-Diindolylmethane 1968-05-4 C17H14N2 246.31
Boldenone Undecylenate 13103-34-9 C30H44O3 452.67
Testosterone 58-22-0 C19H28O2 288.42
Cyproterone (acetate) 427-51-0 0.0
GLPG 0492 1215085-92-9 C19H14F3N3O3 389.33
N-desmethyl Enzalutamide 1242137-16-1 C20H14F4N4O2S 450.41
AZD3514 1240299-33-5 C25H32F3N7O2 519.56
DHEA 53-43-0 C19H28O2 288.42
RAD140 1182367-47-0 C20H16ClN5O2 393.83
17 alpha-propionate 19608-29-8 C24H34O5 402.52
BMS-564929 627530-84-1 C14H12ClN3O3 305.72
MK-0773 606101-58-0 C27H34FN5O2 479.59

Recommended Compounds in Same Indication

Name CAS No Formula MW
TAK-700 (R-form) 752243-39-3 C18H17N3O2 307.35
Olaparib 763113-22-0 C24H23FN4O3 434.46
KX2-391 897016-82-9 C26H29N3O3 431.53
Bicalutamide 90357-06-5 C18H14F4N2O4S 430.37
Enzalutamide 915087-33-1 C21H16F4N4O2S 464.44
Linsitinib 867160-71-2 C26H23N5O 421.49
Fenretinide 65646-68-6 C26H33NO2 391.55
Leuprolide (Acetate) 74381-53-6 C61H88N16O14 1269.45
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
(S)-N-(3-([4,5'-bipyrimidin]-2-ylamino)-4-methylphenyl)-4-((3-(dimethylamino)pyrrolidin-1-yl)methyl)-3-(trifluoromethyl)benzamide 859212-16-1 C30H31F3N8O 576.62
AT13387 912999-49-6 C24H31N3O3 409.52
Tasquinimod 254964-60-8 C20H17F3N2O4 406.36
Orteronel 566939-85-3 C18H17N3O2 307.35
TAK-700 426219-18-3 C18H17N3O2 307.35
TAK-700 (salt) 426219-53-6 C28H28N4O7 532.54
TOK-001 851983-85-2 C26H32N2O 388.55
Cabozantinib 849217-68-1 C28H24FN3O5 501.51
Odanacatib 603139-19-1 C25H27F4N3O3S 525.56
Zibotentan 186497-07-4 C19H16N6O4S 424.43
11

Route of Synthesis

12

References

13

More Information

ARN-509

Tags: buy 956104-40-8 IC50 | 956104-40-8 price | 956104-40-8 cost | 956104-40-8 solubility | 956104-40-8 purchase | 956104-40-8 manufacturer | 956104-40-8 research buy | 956104-40-8 order | 956104-40-8 MSDS | 956104-40-8 chemical structure | 956104-40-8 Storage condition | 956104-40-8 molecular weight | 956104-40-8 mw | 956104-40-8 datasheet | 956104-40-8 supplier | 956104-40-8 cell line | 956104-40-8 NMR | 956104-40-8 MS | 956104-40-8 IR | 956104-40-8 solubility | 956104-40-8 Safe information | 956104-40-8 Qc and Spectral Information | 956104-40-8 Clinical Information | 956104-40-8 Clinical Trial | 956104-40-8 Route of Synthesis | 956104-40-8 storage condition | 956104-40-8 diseases and conditions | 956104-40-8 flash point | 956104-40-8 boiling point | 956104-40-8 melting point | 956104-40-8 storage condition | 956104-40-8 brand