Galeterone
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MedKoo CAT#: 205646

CAS#: 851983-85-2

Description: Galeterone, also known as TOK-001 and NX41765; 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.


Price and Availability

Size Price Shipping out time Quantity
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 650 Same day
500mg USD 1050 Same day
1g USD 1850 Same day
2g USD 3250 Same day
5g USD 4650 2 weeks
10g USD 6450 2 weeks
Inquire bulk and customized quantity

Pricing updated 2020-04-02. Prices are subject to change without notice.

Galeterone, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2g may be 2 weeks.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205646
Name: Galeterone
CAS#: 851983-85-2
Chemical Formula: C26H32N2O
Exact Mass: 388.25146
Molecular Weight: 388.54508
Elemental Analysis: C, 80.37; H, 8.30; N, 7.21; O, 4.12


Synonym: TOK001; TOK 001; TOK-001; NX41765; NX 41765; NX-41765; VN 1241; VN-1241; VN-1241; Galeterone.

IUPAC/Chemical Name: (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

InChi Key: PAFKTGFSEFKSQG-PAASFTFBSA-N

InChi Code: InChI=1S/C26H32N2O/c1-25-13-11-18(29)15-17(25)7-8-19-20-9-10-24(26(20,2)14-12-21(19)25)28-16-27-22-5-3-4-6-23(22)28/h3-7,10,16,18-21,29H,8-9,11-15H2,1-2H3/t18-,19-,20-,21-,25-,26-/m0/s1

SMILES Code: O[C@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)C(N5C=NC6=CC=CC=C56)=CC[C@@]4([H])[C@]3([H])CC=C2C1


Technical Data

Appearance:
White to off white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

 Galeterone (TOK-001 or VN/124-1) is a novel antiandrogen under development by Tokai Pharmaceuticals for the treatment of prostate cancer. It possesses a unique dual mechanism of action, acting as both an androgen receptor antagonist and an inhibitor of CYP17A1, an enzyme required for the biosynthesis of the androgens.  As of the second half of 2014, galeterone is in phase III clinical trials for castration-resistant prostate cancer.

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: Gomez L, Kovac JR, Lamb DJ. CYP17A1 inhibitors in castration-resistant prostate cancer. Steroids. 2015 Jan 3. pii: S0039-128X(14)00314-6. doi: 10.1016/j.steroids.2014.12.021. [Epub ahead of print] PubMed PMID: 25560485.

2: Gupta E, Guthrie T, Tan W. Changing paradigms in management of metastatic Castration Resistant Prostate Cancer (mCRPC). BMC Urol. 2014 Jul 25;14:55. doi: 10.1186/1471-2490-14-55. PubMed PMID: 25062956; PubMed Central PMCID: PMC4167156.

3: Yu Z, Cai C, Gao S, Simon NI, Shen HC, Balk SP. Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor. Clin Cancer Res. 2014 Aug 1;20(15):4075-85. doi: 10.1158/1078-0432.CCR-14-0292. Epub 2014 May 29. PubMed PMID: 24874833; PubMed Central PMCID: PMC4119496.

4: Stein MN, Patel N, Bershadskiy A, Sokoloff A, Singer EA. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400. doi: 10.4103/1008-682X.129133. Review. PubMed PMID: 24759590; PubMed Central PMCID: PMC4023364.

5: Agarwal N, Di Lorenzo G, Sonpavde G, Bellmunt J. New agents for prostate cancer. Ann Oncol. 2014 Sep;25(9):1700-9. doi: 10.1093/annonc/mdu038. Epub 2014 Mar 20. PubMed PMID: 24658665.

6: Neuzillet Y, Flamand V, Lebdai S, Villers A, Lebret T. [Prostate cancer and new hormonal treatments: mechanism of action and main clinical results]. Prog Urol. 2013 Oct;23 Suppl 1:S34-43. doi: 10.1016/S1166-7087(13)70044-7. Review. French. PubMed PMID: 24314737.

7: Yin L, Hu Q. CYP17 inhibitors--abiraterone, C17,20-lyase inhibitors and multi-targeting agents. Nat Rev Urol. 2014 Jan;11(1):32-42. doi: 10.1038/nrurol.2013.274. Epub 2013 Nov 26. Review. PubMed PMID: 24276076.

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