Name: MDV3100 (Enzalutamide)
Brand: Selleck Chemicals
SKU: S1250
Rating: 5 (556 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.99%

99.99

관련 타겟	Adrenergic Receptor Estrogen/progestogen Receptor GPR Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
기타 Androgen Receptor 억제제	Bavdegalutamide (ARV-110) RU58841 EPI-001 Galeterone Cyproterone Acetate 3,3'-Diindolylmethane Ailanthone JNJ-63576253 (TRC-253) Proxalutamide (GT0918) AZD3514

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주	분석 유형	농도	배양 시간	제형	활성 설명	PMID
human LNCAP	Cytotoxic Assay		7 days	95% EtOH	IC50=5.12 μM	23713567
human LNCAP	Function Assay	1 μM		DMSO	Inhibits prostate specific antigen secretion in human LNCAP cells expressing androgen receptor at 100-1000nM	20218717
VCaP	Function Assay	10 μM	24 h	DMSO	Suppresses ligand-mediated AR-FL signaling	22710436
BCK4	Function Assay	10 μM	7 days	DMSO	Inhibits estradiol-mediated proliferation	24451109
MCF7s	Function Assay	10 μM	6 days	DMSO	Inhibits estradiol-mediated proliferation	24451109
PC-3	Function Assay	10 μM	72 h	DMSO	Does not inhibit cell proliferation	25344864
CWR22Rv1	Function Assay	15 μM	24 h	DMSO	Does not affect the full length AR expression	23713567
LNCAP/AR	Antagonist activity assay				IC50 = 0.021 μM	27717544
MDA-MB-453	Antagonist activity assay				EC50 = 0.049 μM	23713567
LNCAP	Antagonist activity assay		72 h		IC50 = 0.05 μM	30193215
LNCAP	Antagonist activity assay		72 h		IC50 = 0.09 μM	30193215
LNCAP	Growth inhibition assay				GI50 = 0.12 μM	28011219
LNCAP	Antiproliferative activity assay		3 days		IC50 = 0.1271 μM	26046313
LNCAP	Antagonist activity assay		6 days		GI50 = 0.29 μM	28011219
UAS-bla GripTite 293	Antagonist activity assay		16 to 24 h		IC50 = 0.361 μM	27301368
mammalian expression system	Antagonist activity assay		22 to 24 h		EC50 = 0.42 μM	28385503
VCaP	Growth inhibition assay		144 h		GI50 = 0.61 μM	25121586
LNCaP	Antagonist activity assay		2 h		EC50 = 0.915 μM	23713567
COS7	Antagonist activity assay		24 h		IC50 = 1.26 μM	29117897
AR LBD mutant	Antagonist activity assay		4 h		IC50 = 1.35 μM	27810589
LNCAP	Growth inhibition assay				GI50 = 2.88 μM	25634130
CWR22Rv1	Growth inhibition assay				GI50 = 3.34 μM	25634130
LNCAP	Cytotoxicity assay		7 days		GI50 = 5.12 μM	23713567
PC3	Growth inhibition assay				GI50 = 9.15 μM	25634130
CWR22Rv1	Cell survival assay		144 h		IC50 = 9.7 μM	25121586
LNCAP	Antiproliferative activity assay		96 h		IC50 = 11.47 μM	27301368
LNCaP-hr	Antiproliferative activity assay		3 days		IC50 = 12.5 μM	27810589
LNCAP	Antiproliferative activity assay		3 days		IC50 = 12.5 μM	29117897
LNCaP	Antagonist activity assay		144 h		GI50 = 18.88 μM	28272894
LNCaP-AR	Growth inhibition assay		144 h		GI50 = 18.9 μM	25121586
C4-2B	Antiproliferative activity assay		12 h		IC50 = 20.77 μM	29758518
A31	Growth inhibition assay		72 h		GI50 = 27.5 μM	28011219
22Rv1	Antiproliferative activity assay		96 h		IC50 = 31.76 μM	27301368
22Rv1	Antiproliferative activity assay		96 h		IC50 = 31.76 μM	26965862
DU145	Antiproliferative activity assay		96 h		IC50 = 32.27 μM	27301368
LNCAP	Antiproliferative activity assay		72 h		IC50 = 33.84 μM	29448139
CW22Rv1	Antagonist activity assay		72 h		IC50 = 35.75 μM	28272894
22Rv1	Antiproliferative activity assay		72 h		IC50 = 36.66 μM	29448139
22Rv1	Antiproliferative activity assay		12 h		IC50 = 36.66 μM	29758518
LNCAP	Antiproliferative activity assay		12 h		IC50 = 42.37 μM	29758518
DU145	Antiproliferative activity assay		3 days		IC50 = 46.1 μM	27810589
DU145	Antiproliferative activity assay		3 days		IC50 = 46.1 μM	29117897
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	464.44	화학식	C₂₁H₁₆F₄N₄O₂S	보관 (수령일로부터)	3년-20°C분말
CAS 번호	915087-33-1	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	MDV3100			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

용해도 (Solubility)

In vitro
배치:

DMSO : 92 mg/mL (198.08 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 24 mg/mL

Water : Insoluble

DMSO : 92 mg/mL (198.08 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 92 mg/mL (198.08 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (200.24 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 4 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.500mg/ml (3.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	2.500mg/ml (5.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC₅₀/Ki	Androgen Receptor (LNCaP cells) 36 nM
시험관 내(In vitro)	Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[¹⁸F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While this compound shows no agonism in LNCaP/AR prostate cells. It antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. This chemical could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp⁷⁴¹ to Cys). It also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex.
키나아제 분석	AR reporter assay
키나아제 분석	Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of this compound is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to this compound treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of this chemical. After two days of incubation, reporter activities are assayed.
생체 내(In vivo)	Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/19359544/ [2] https://pubmed.ncbi.nlm.nih.gov/20398925/ [3] http://worldwide.espacenet.com/publicationDetails/originalDocument?CC=US&NR=2007254933A1&KC=A1&FT=D&

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7 AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166) CXCR7	28607007
Growth inhibition assay	Cell proliferation	28115200
Immunofluorescence	AR pAKT(S473) CXCR7	27588408
ELISA	osteoprotegerin	27015557

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT06130995	Not yet recruiting	Androgen Deprivation Therapy\|Locally Advanced Prostate Cancer	University of Oklahoma	August 2024	Phase 1
NCT05339672	Recruiting	Drug-drug Interaction	Radboud University Medical Center\|Astellas Pharma Inc	July 1 2024	--
NCT06096870	Recruiting	Prostate Cancer\|Recurrent Prostate Cancer\|PET Positive	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	April 22 2024	Phase 2
NCT05743621	Recruiting	Prostatic Neoplasms Castration-Resistant	Weill Medical College of Cornell University\|Sagimet Biosciences Inc.	November 20 2023	Phase 1

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

MDV3100 (Enzalutamide) Androgen Receptor antagonist

화학 구조

분자량: 464.44

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

MDV3100 (Enzalutamide) Androgen Receptor antagonist

화학 구조

분자량: 464.44

품질 관리 (Quality Control)

세포 배양, 처리 및 작업 농도 (Cell Culture, Treatment & Working Concentration)

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)