엔잘루타마이드

한글명:엔잘루타마이드

카스 번호915087-33-1

상품명:Enzalutamide

CBNumberCB62500946

분자식C21H16F4N4O2S

포뮬러 무게464.44

MOL 파일915087-33-1.mol

동의어(한글)

엔잘루타마이드

화학적 성질

녹는점	198 - 200°C
밀도	1.49
저장 조건	-20°C
용해도	DMSO에 용해됨(>25 mg/ml)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	13.88±0.46(Predicted)
색상	흰색에서 황백색까지
안정성	공급된 대로 1년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
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)
InChIKey	WXCXUHSOUPDCQV-UHFFFAOYSA-N
SMILES	C(NC)(=O)C1=CC=C(N2C(=S)N(C3=CC=C(C#N)C(C(F)(F)F)=C3)C(=O)C2(C)C)C=C1F

위험 및 안전 성명

HS 번호

29339900

NFPA 704:

	0
2		0

그림문자(GHS)

엔잘루타마이드 화학적 특성, 용도, 생산

개요
In August 2012, the US FDA approved enzalutamide for the treatment of metastatic castration-resistant prostate cancer (mCRPC) in patients who have previously been treated with docetaxel. Synthesis of enzalutamide was achieved by a triply convergent route that employed a Strecker condensation, followed by isothiocyanate condensation and hydrolysis to form the thiohydantoin moiety. In LNCaP/AR cells with high expression of AR, enzalutamide demonstrated potent inhibition of 16b-[18F]-5α-dihydrotestosterone binding (IC₅₀=21 nM compared with bicalutamide IC₅₀=160 nM), and inhibited AR translocation to the nucleus more potently than bicalutamide.The primary metabolite is the result of CYP2C8-mediated N-demethylation; enzalutamide is primarily eliminated by hepatic metabolism.
화학적 성질
White Solid
용도
MDV3100, known as Enzalutamide, is a second-generation androgen receptor (AR) signaling inhibitor. It is able to inhibit binding of androgens to the AR, AR nuclear translocation, and the association of the AR with DNA.
정의
ChEBI: A benzamide obtained by formal condensation of the carboxy group of 4-{3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl}-2-fluorobenzoic acid with methylamine. Used for the treatment of of metastatic castration-resistant p ostate cancer.
Clinical Use
In August 2012, the FDA approved enzalutamide, marketed by Medivation and Astellas Pharma US for the treatment of metastatic castration-resistant prostate cancer (CRPC), specifically for those patients who had previously received docetaxel. Enzalutamide is an inhibitor of androgen receptors (AR)— whose increased expression has been closely linked with castration-resistant prostate cancer (CRPC),thus, AR inhibitors have seen increased recent attention from the medicinal chemistry community. Phase I/II trials were particularly promising for enzalutamide, as 43% of patients showed >50% sustained suppression of a key serum biomarker.

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