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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-Gumelutamide
Gumelutamide

Chemical Structure : Gumelutamide

CAS No.: 1831085-48-3

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Gumelutamide (TAS-3681, TAS3681)

货号: PC-20039Not For Human Use, Lab Use Only.

Gumelutamide (TAS3681) is a potent, selective androgen receptor (AR) pure antagonist with Ki of 7.39 and 23.8 nM for WT AR and AR T878A mutant respectively, inhibits AR transcriptional activity and downregulates AR-full length (AR-FL) and AR-Vs.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Gumelutamide (TAS3681) is a potent, selective androgen receptor (AR) pure antagonist with Ki of 7.39 and 23.8 nM for WT AR and AR T878A mutant respectively, inhibits AR transcriptional activity and downregulates AR-full length (AR-FL) and AR-Vs.
TAS3681 is a potent antagonist for wild-type AR with IC50 values of 52.7 and 60.9  nM, respectively, for COS-7 cells and VCaP cells that express wild-type AR in AR transactivation assays.
TAS3681 dose-dependently suppresses LNCaP cell proliferation with IC50 of 18 nM, inhibits DHT-induced cell proliferation more potently than bicalutamide, and with activity similar to enzalutamide.
TAS3681 impairs nuclear translocation and DNA binding of AR in prostate cancer cells.
TAS3681 is a pure antagonist for AR-LBD mutants (mutated ARs L702H, V716M, W742L, H875Q, H875Y, D891Y, Q903H, H875Y/T878A, T878A/S889G, and T878A/D891H).
TAS3681 reduces AR protein levels and suppresses AR transactivation and growth of AR-overexpressing enzalutamide-resistant cells, downregulates both AR-FL and AR-V7 protein levels at the translational level.
TAS3681 (7.5, 15, or 22.5  mg/kg, oral, twice daily) suppresses tumor growth in enzalutamide-resistant PCa xenograft.

物理化学性质&存储条件

分子量 420.90
分子式 C22H21ClN6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-chloro-4-(4-((5-(2-hydroxypropan-2-yl)pyridin-2-yl)amino)-5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl)benzonitrile

参考文献

1. Patent WO2022212631 A1.
2. Yoshida S, et al. Mol Oncol. 2024 Apr 10. doi: 10.1002/1878-0261.13641.

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