Galeterone
- CAS No.
- 851983-85-2
- Chemical Name:
- Galeterone
- Synonyms
- VN 124;CS-232;TOK-001;NX41765;VN/124-1;Galeterone;Galaterone;synthesis-008;synthesis-1-007;TOK-001 impurity
- CBNumber:
- CB32500945
- Molecular Formula:
- C26H32N2O
- Molecular Weight:
- 388.55
- MOL File:
- 851983-85-2.mol
- Modify Date:
- 2024/1/4 11:05:08
| Melting point | 189-190℃ |
|---|---|
| Boiling point | 564.5±60.0 °C(Predicted) |
| Density | 1.28 |
| storage temp. | -20°C Freezer |
| solubility | Chloroform (Slightly), Ethyl Aceatae (Slightly, Heated) |
| pka | 14.71±0.70(Predicted) |
| form | Solid |
| color | 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| |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Danger |
| Hazard statements | H361 |
| Precautionary statements | P201-P202-P281-P308+P313-P405-P501 |
Galeterone price More Price(2)
Galeterone Chemical Properties,Uses,Production
Description
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.
Uses
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.
Biological Activity
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 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 | China | 29798 | 60 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32836 | 60 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49392 | 58 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29825 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 24200 | 58 | Inquiry |
| AFINE CHEMICALS LIMITED | +86-0571-85134551 | China | 15395 | 58 | Inquiry |
| Supplier | Advantage |
|---|---|
| CLEARSYNTH LABS LTD. | 58 |
| A.J Chemicals | 58 |
| Capot Chemical Co.,Ltd. | 60 |
| ATK CHEMICAL COMPANY LIMITED | 60 |
| BOC Sciences | 58 |
| Chongqing Chemdad Co., Ltd | 58 |
| CONIER CHEM AND PHARMA LIMITED | 58 |
| career henan chemical co | 58 |
| Dideu Industries Group Limited | 58 |
| AFINE CHEMICALS LIMITED | 58 |