1831085-48-3
Chemical Structure
Gumelutamide
Synonym(s): TAS3681
- CAS No.: 1831085-48-3
- Formula:C22H21ClN6O
- Molecular Weight:420.89
IUPAC Name: 6-(((R)-2-hydroxy-2-methylbut-3-yn-1-yl)oxy)-4-(6-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile
InChIKey: TYOPGJVWUJIKHX-UHFFFAOYSA-N
SMILES: N#CC1=CC=C(N2CC3=C(CC2)C(NC4=NC=C(C(C)(C)O)C=C4)=NC=N3)C=C1Cl
Biological Activity: Gumelutamide (TAS3681) is an orally active androgen receptor (AR) antagonist with an IC50 of 52.7 nM in COS-7 cells. Gumelutamide binds to AR, blocks nuclear translocation and DNA binding, and antagonizes full-length AR, AR mutants, and AR splice variants. Gumelutamide induces apoptosis and inhibits androgen-dependent proliferation in AR-positive prostate cancer cells. Gumelutamide can be used in research on metastatic castration-resistant prostate cancer and prostate cancer[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Gumelutamide | 99.00% | Gumelutamide (TAS3681) is an orally active androgen receptor (AR) antagonist with an IC50 of 52.7 nM in COS-7 cells. Gumelutamide binds to AR, blocks nuclear translocation and DNA binding, and antagonizes full-length AR, AR mutants, and AR splice variants. Gumelutamide induces apoptosis and inhibits androgen-dependent proliferation in AR-positive prostate cancer cells. Gumelutamide can be used in research on metastatic castration-resistant prostate cancer and prostate cancer. | ||||||||||||||||||||
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Similarity Score 0.87
HY-152850AGumelutamide monosuccinate -
Similarity Score 0.47
HY-146205ATX inhibitor 18 -
Similarity Score 0.46
HY-133019ATX inhibitor 5 -
Similarity Score 0.46
HY-118172PD-307243 -
Similarity Score 0.46
HY-124310PDE5-IN-6c -
Similarity Score 0.45
HY-131063CDK6/9-IN-1 -
Similarity Score 0.45
HY-150974ROS1-IN-1 -
Similarity Score 0.44
HY-123129RS 2232 -
Similarity Score 0.44
HY-400666AR ligand-44 -
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References
- [1]. Bernard-Tessier A, et al. The future of androgen receptor targeting in prostate cancer: third-generation inhibitors and beyond. Ther Adv Med Oncol. 2025 Sep 29;17:17588359251379416.
- [2]. World Health Organization. International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 128. WHO Drug Information. 2022;36(4).
- [3]. Yoshida S, et al. TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer. Molecular oncology. 2024 Aug;18(8):1980-2000. [Content Brief]
