Gumelutamide (TAS3681) | AR inhibitor | Probechem Biochemicals

Chemical Structure : Gumelutamide

CAS No.: 1831085-48-3

Gumelutamide (TAS-3681, TAS3681)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	420.90
Formula	C22H21ClN6O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

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

Gumelutamide (TAS-3681, TAS3681)

Biological Activity

Physicochemical Properties

References

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