Galeterone

한글명:Galeterone

카스 번호851983-85-2

상품명:Galeterone

CBNumberCB32500945

분자식C26H32N2O

포뮬러 무게388.55

MOL 파일851983-85-2.mol

화학적 성질

녹는점	189-190℃
끓는 점	564.5±60.0 °C(Predicted)
밀도	1.28
저장 조건	-20°C Freezer
용해도	클로로포름(약간), 아세트산에틸(약간, 가열)에 용해됨
산도 계수 (pKa)	14.71±0.70(Predicted)
물리적 상태	고체
물리적 상태	단단한 모양
색상	흰색에서 황백색까지
InChIKey	PAFKTGFSEFKSQG-MRFMOSGMNA-N
SMILES	C1C[C@]2(C)C3CC[C@]4(C)C([n]5cnc6ccccc56)=CCC4C3CC=C2C[C@H]1O \|&1:2,7,27,r\|

그림문자(GHS)

Galeterone 화학적 특성, 용도, 생산

개요
Galeterone (TOK-001) is a small molecule oral drug that disrupts AR signaling by a novel triple mechanism: it potently and selectively inhibits CYP17 lyase, potently antagonizes AR and decreases AR protein levels (wild-type and mutant), leading to antitumor activity. Galeterone has shown significant anti-tumour activity with a well-tolerated safety profile in patients with CRPC in phase I and II clinical studies.
용도
Galeterone is an androgen receptor antagonist and CYP17A1 enzyme inhibitor. It has been used in trials studying the treatment of Prostate Cancer.
정의
ChEBI: Galeterone is a 3-hydroxy steroid. It has a role as an androgen.
생물학적 활성
The cytochrome P450 (CYP) isoform CYP17 is also known as steroid 17α-hydroxylase/17,20 lyase because it catalyzes both 17α-hydroxylase and 17,20 lyase reactions in the synthesis of steroids, including androgens, estrogens, glucocorticoids, and mineralocorticoids. Galeterone is a CYP17 inhibitor (IC50 = 300 nM) that has been shown to competitively block synthetic androgen binding (EC50 = 845 nM) and to antagonize the androgen receptor in transcriptional activation assays. Galeterone can inhibit the growth of castration-resistant prostate cancer cells with an IC50 value of 2.9 μM and demonstrates synergy with everolimus or gefitinib for growth inhibition.
Mode of action
Galeterone is an orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens.

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