A CYP17 inhibitor
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Galeterone

Item No. 17586

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
17-(1H-benzimidazol-1-yl)-androsta-5,16-dien-3β-ol
CAS Number
851983-85-2
Synonyms
  • TOK-001
Molecular Formula
C26H32N2O
Formula Weight
388.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2)(1:3): 0.2 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/ml
SMILES
C[C@@]12[C@](CC=C2N3C(C=CC=C4)=C4N=C3)([H])[C@]5([H])CC=C6C[C@@H](O)CC[C@]6(C)[C@@]5([H])CC1
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
InChi Key
PAFKTGFSEFKSQG-PAASFTFBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $28

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    5 mg

    $97

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    10 mg

    $152

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    25 mg

    $238

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    Product Description

    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.1 Galeterone can inhibit the growth of castration-resistant prostate cancer cells with an IC50 value of 2.9 µM and demonstrates synergy with everolimus (Item No. 11597) or gefitinib (Item No. 13166) for growth inhibition.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Njar, V.C.O., and Brodie, A.M.H. Discovery and development of galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer. J. Med. Chem. 58(5), 2077-2087 (2015).

    2. Gupta, E., Guthrie, T., and Tan, W. Changing paradigms in management of metastatic Castration Resistant Prostate Cancer (mCRPC). BMC Urol. 14, 55 (2014).