Galeterone

Product Name: Galeterone
CAS No.: 851983-85-2
Chemical Name: Galeterone
Synonyms: VN 124;CS-232;NX41765;TOK-001;VN/124-1;Galeterone;Galaterone;synthesis-008;synthesis-1-007;TOK-001 impurity
CBNumber: CB32500945
Molecular Formula: C26H32N2O
Formula Weight: 388.55
MOL File: 851983-85-2.mol

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Galeterone Property

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|

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1375
Product name: Galeterone
Purity: ≥98% (HPLC)
Packaging: 5MG
Price: $91.9
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML1375
Product name: Galeterone
Purity: ≥98% (HPLC)
Packaging: 25MG
Price: $370
Updated: 2024/03/01

Cayman Chemical

Product number: 17586
Product name: Galeterone
Purity: ≥98%
Packaging: 1mg
Price: $25
Updated: 2024/03/01

Cayman Chemical

Product number: 17586
Product name: Galeterone
Purity: ≥98%
Packaging: 5mg
Price: $88
Updated: 2024/03/01

Cayman Chemical

Product number: 17586
Product name: Galeterone
Purity: ≥98%
Packaging: 10mg
Price: $138
Updated: 2024/03/01

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Galeterone Chemical Properties,Usage,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.

target

CYP17

storage

Store at -20°C

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.

References

[1]. devore n m, & scott e e. structures of cytochrome p450 17a1 with prostate cancer drugs abiraterone and tok-001. nature, 2012, 482: 116-119.
[2]. mallik i, davila m, tapia t, et al. androgen regulates cdc6 transcription through interactions between androgen receptor and e2f transcription factor in prostate cancer cells. biochimica et biophysica acta (bba) - molecular cell research, 2008,1783:1737-1744.
[3]. bruno r d, vasaitis t s, gediya l. k, et al. synthesis and biological evaluations of putative metabolically stable analogs of vn/124-1 (tok-001): head to head anti-tumor efficacy evaluation of vn/124-1 (tok-001) and abiraterone in lapc-4 human prostate cancer xenograft model. steroids, 2011,76: 1268-1279.

Galeterone Preparation Products And Raw materials

Raw materials

Preparation Products

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Galeterone Suppliers

Canada 1 China 125 India 2 United Kingdom 3 United States 15 Global 146

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4861
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AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2782
Advantage: 58

Target molecule Corp.

Tel: 857-239-0968
Fax: 857-239-8801
Email: service1@targetmol.com
Country: United States
ProdList: 2559
Advantage: 60

Musechem

Tel: +1-800-259-7612
Fax: +1-800-259-7612
Email: info@musechem.com
Country: United States
ProdList: 4660
Advantage: 60

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 32165
Advantage: 58

InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6391
Advantage: 58

Cckinase, Inc.

Tel: +1 (732)236-3202
Email: sales@cckinase.com
Country: United States
ProdList: 2738
Advantage: 58

BOC Sciences

Tel: +1-631-485-4226
Fax: 1-631-614-7828
Email: inquiry@bocsci.com
Country: United States
ProdList: 19553
Advantage: 58

Aladdin Scientific

Tel: +1-+1(833)-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 57505
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TargetMol Chemicals Inc.

Tel
Email: support@targetmol.com
Country: United States
ProdList: 38632
Advantage: 58

ApexBio Technology

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Email: sales@apexbt.com
Country: United States
ProdList: 6251
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Cayman Chemical Company

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Country: United States
ProdList: 6213
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United States Biological

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Country: United States
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AK Scientific, Inc.

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Country: United States
ProdList: 6347
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Santa Cruz Biotechnology, Inc.

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Country: United States
ProdList: 3597
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View Lastest Price from Galeterone manufacturers

Shenzhen Nexconn Pharmatechs Ltd

Product: Galeterone 851983-85-2
Price: US $200.00-3000.00/g
Min. Order: 1g
Purity: 98%
Supply Ability: 1kg
Release date: 2024-01-03

Career Henan Chemical Co

Product: Galeterone 851983-85-2
Price: US $6.68/KG
Min. Order: 1KG
Purity: 97%-99%
Supply Ability: 1kg-1000kg
Release date: 2020-01-08

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(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

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

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

851983-85-2

Inhibitors

API