Enzalutamide - ≥98%, high purity , Androgen Receptor antagonist, CAS No.915087-33-1, Androgen Receptor antagonist

1 Citations
Item Number
E127109
Grouped product items
SKUSizeAvailabilityPrice Qty
E127109-25mg
25mg
In stock
$56.90
E127109-100mg
100mg
In stock
$187.90
E127109-200mg
200mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$418.90
E127109-250mg
250mg
In stock
$423.90
E127109-1g
1g
In stock
$533.90
E127109-5g
5g
In stock
$1,711.90
View related series
Androgen receptor Antagonist

Basic Description

SynonymsMDV3100 | AMY10296 | Xtandi (TN) | FT-0673286 | MDV-3100;Enzalutamide;MDV 3100 | Benzamide, 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-methyl- | MFCD14155804 | AB01565849_02 | FT-0670957 | HY-70002 |
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsMDV3100 is an androgen receptor inhibitor and antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2) in combination with the synthetic androgen R1881 in parental LNCaP cells. MDV3100 prevents nuclear translo
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAndrogen Receptor antagonist
Product Description

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
An androgen receptor inhibitor

Product Properties

ALogP3.6

Associated Targets(Human)

KLK3 Tclin Prostate-specific antigen (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AR Tclin Androgen receptor (12 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
F2 Tclin Thrombin (11687 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ESR1 Tclin Estrogen receptor alpha (17718 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PGR Tclin Progesterone receptor (8562 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR3C2 Tclin Mineralocorticoid receptor (2134 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AR Tclin Androgen Receptor (11781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CACNA1C Tclin Voltage-gated L-type calcium channel alpha-1C subunit (766 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TBXA2R Tclin Thromboxane A2 receptor (5717 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE4A Tclin Phosphodiesterase 4A (1943 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Npy1r Neuropeptide Y receptor type 1 (8 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cckar Cholecystokinin A receptor (90 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pde4d Phosphodiesterase 4D (4 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NIH3T3 (5395 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gabrp GABA-A receptor; anion channel (5731 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name 4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluoro-N-methylbenzamide
INCHI InChI=1S/C21H16F4N4O2S/c1-20(2)18(31)28(12-5-4-11(10-26)15(8-12)21(23,24)25)19(32)29(20)13-6-7-14(16(22)9-13)17(30)27-3/h4-9H,1-3H3,(H,27,30)
InChi Key WXCXUHSOUPDCQV-UHFFFAOYSA-N
Canonical SMILES CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
Isomeric SMILES CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
Alternate CAS 915087-33-1
PubChem CID 15951529
MeSH Entry Terms 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-(methyl-d3)benzamide;4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-methyl-benzamide;enzalutamide;enzaluta
Molecular Weight 464.44

Certificates

Certificate of Analysis(COA)

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19 results found

Lot NumberCertificate TypeDateItem
I2228198Certificate of AnalysisJul 05, 2024 E127109
F2224030Certificate of AnalysisApr 03, 2024 E127109
F2224029Certificate of AnalysisApr 03, 2024 E127109
B2215264Certificate of AnalysisDec 12, 2023 E127109
B2215238Certificate of AnalysisDec 12, 2023 E127109
L2114014Certificate of AnalysisSep 21, 2023 E127109
L1904046Certificate of AnalysisJul 06, 2023 E127109
C2111198Certificate of AnalysisDec 15, 2022 E127109
A2306523Certificate of AnalysisOct 18, 2022 E127109
A2306527Certificate of AnalysisOct 18, 2022 E127109
A2306528Certificate of AnalysisOct 18, 2022 E127109
A2306517Certificate of AnalysisOct 18, 2022 E127109
A2306513Certificate of AnalysisOct 18, 2022 E127109
A2306510Certificate of AnalysisOct 18, 2022 E127109
A2306505Certificate of AnalysisOct 18, 2022 E127109
A2306489Certificate of AnalysisOct 18, 2022 E127109
A2306477Certificate of AnalysisOct 18, 2022 E127109
B2215241Certificate of AnalysisDec 27, 2021 E127109
B2215246Certificate of AnalysisDec 27, 2021 E127109

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Chemical and Physical Properties

SolubilityDMSO ≥90mg/mL Water <1.2mg/mL Ethanol ≥15mg/mL

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS09,   GHS07
Signal Danger
Hazard Statements

H373:Causes damage to organs through prolonged or repeated exposure

H411:Toxic to aquatic life with long lasting effects

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

H360D:May damage 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.

Related Documents

Citations of This Product

1. Jiang, Zhihui Z, Zhou, Bo B, Li, Xinping X, Kirby, Gordon M GM and Zhang, Xiaoying X..  (2018)  Echinacoside Increases Sperm Quantity in Rats by Targeting the Hypothalamic Androgen Receptor..  Scientific reports,    (1):   [PMID:29497114]

References

1. Beer TM, Armstrong AJ, Rathkopf DE, Loriot Y, Sternberg CN, Higano CS, Iversen P, Bhattacharya S, Carles J, Chowdhury S et al..  (2014)  Enzalutamide in metastatic prostate cancer before chemotherapy..  N Engl J Med,  371  (5): (424-33).  [PMID:24881730]
2. Hussain M, Fizazi K, Saad F, Rathenborg P, Shore N, Ferreira U, Ivashchenko P, Demirhan E, Modelska K, Phung et al..  (2018)  Enzalutamide in Men with Nonmetastatic, Castration-Resistant Prostate Cancer..  N Engl J Med,  378  (26): (2465-2474).  [PMID:29949494]
3. Armstrong AJ, Szmulewitz RZ, Petrylak DP, Holzbeierlein J, Villers A, Azad A, Alcaraz A, Alekseev B, Iguchi T, Shore ND et al..  (2019)  ARCHES: A Randomized, Phase III Study of Androgen Deprivation Therapy With Enzalutamide or Placebo in Men With Metastatic Hormone-Sensitive Prostate Cancer..  J Clin Oncol,  37  (32): (2974-2986).  [PMID:31329516]
4. Jiang, Zhihui Z, Zhou, Bo B, Li, Xinping X, Kirby, Gordon M GM and Zhang, Xiaoying X..  (2018)  Echinacoside Increases Sperm Quantity in Rats by Targeting the Hypothalamic Androgen Receptor..  Scientific reports,    (1):   [PMID:29497114]

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