Galeterone
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- CAS-Nr.
- 851983-85-2
- Englisch Name:
- Galeterone
- Synonyma:
- VN 124;CS-232;TOK-001;NX41765;VN/124-1;Galeterone;Galaterone;synthesis-008;synthesis-1-007;TOK-001 impurity
- CBNumber:
- CB32500945
- Summenformel:
- C26H32N2O
- Molgewicht:
- 388.55
- MOL-Datei:
- 851983-85-2.mol
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Galeterone Eigenschaften
- Schmelzpunkt:
- 189-190℃
- Siedepunkt:
- 564.5±60.0 °C(Predicted)
- Dichte
- 1.28
- storage temp.
- -20°C Freezer
- L?slichkeit
- Chloroform (Slightly), Ethyl Aceatae (Slightly, Heated)
- pka
- 14.71±0.70(Predicted)
- Aggregatzustand
- Solid
- Farbe
- White to Off-White
- 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|
Sicherheit
- Risiko- und Sicherheitserkl?rung
- Gefahreninformationscode (GHS)
| Bildanzeige (GHS) |
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| Alarmwort |
Achtung |
| Gefahrenhinweise |
| Code |
Gefahrenhinweise |
Gefahrenklasse |
Abteilung |
Alarmwort |
Symbol |
P-Code |
| H361 |
Kann vermutlich die Fruchtbarkeit beeintr?chtigen oder das Kind im Mutterleib sch?digen. |
Reproduktionstoxizit?t |
Kategorie 2 |
Warnung |
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P201, P202, P281, P308+P313, P405,P501 |
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| Sicherheit |
| P201 |
Vor Gebrauch besondere Anweisungen einholen. |
| P202 |
Vor Gebrauch alle Sicherheitshinweise lesen und verstehen. |
| P281 |
Vorgeschriebene pers?nliche Schutzausrüstung verwenden. |
| P308+P313 |
BEI Exposition oder falls betroffen: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen. |
| P405 |
Unter Verschluss aufbewahren. |
| P501 |
Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen. |
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Galeterone Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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.
Verwenden
Galeterone is an androgen receptor antagonist and CYP17A1 enzyme inhibitor. It has been used in trials studying the treatment of Prostate Cancer.
Definition
ChEBI: Galeterone is a 3-hydroxy steroid. It has a role as an androgen.
Biologische Aktivit?t
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.
Galeterone Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Galeterone Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 156)Lieferanten
851983-85-2()Verwandte Suche:
- NX41765
- (3S,8R,9S,10R,13S,14S)-17-(1H-Benzo[d]imidazol-1-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
- (3beta)-17-(1H-Benzimidazol-1-yl)androsta-5,16-dien-3-ol
- Galeterone
- VN 124
- TOK-001 (Galeterone)
- Galeterone,TOK-001
- (3S,10R,13S)-17-(1H-benzo[d]imidazol-1-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol
- TOK-001
- VN/124-1
- Androsta-5,16-dien-3-ol, 17-(1H-benzimidazol-1-yl)-, (3β)-
- GALETERONE;TOK001;TOK 001;TOK-001
- TOK-001 impurity
- (3β)-17-(1H-Benzimidazol-1-yl)androsta-5,16-dien-3-ol
- (3S,8R,9S,10R,13S,14S)-17-(benzimidazol-1-yl)-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-3-ol
- CS-232
- VN/124-1; GALETERONE;TOK001;TOK 001;TOK-001
- Galaterone
- synthesis-008
- synthesis-1-007
- Galeterone USP/EP/BP
- TOK-001/Galeterone,VN/124-1
- Androsta-?5,?16-?dien-?3-?ol, 17-?(1H-?benzimidazol-?1-?yl)?-?, (3β)?-
- Galeterone, TOK-001, VN-124-1
- Galeterone, 10 mM in DMSO
- Galeterone Impurity1
- 851983-85-2
- Inhibitors
- API
