2952994-34-0
Chemical Structure
YXG-158
- CAS No.: 2952994-34-0
- Formula:C30H36FN3O
- Molecular Weight:473.62
InChIKey: JHVKBJJTUMIPIT-SUAVODKESA-N
SMILES: C[C@@]12[C@](CC=C2N3C=C(N=C3)C)([H])[C@@]4([H])[C@@](CC1)([H])[C@@]5(C(C[C@H](CC5)NC(C6=CC=C(C=C6)F)=O)=CC4)C
Biological Activity: YXG‑158 is an orally active, anticancer bifunctional steroid analog with both androgen receptor (AR) degradation activity (DC50 = 1.28 μM) and CYP17A1 inhibitory activity (IC50 = 100 nM). YXG-158 reduces AR protein and mRNA expression via proteasome-dependent degradation, degrades AR-V7, and inhibits CYP17A1 enzymatic activity to block androgen biosynthesis. YXG-158 inhibits the activities of ERα and ERβ, as well as cancer cell proliferation. YXG-158 decreases the weight of androgen-sensitive organs in castrated rats treated with testosterone propionate, downregulates AR protein, reduces PSA levels, and suppresses tumor growth in Enzalutamide (HY-70002)-sensitive and -resistant xenograft models. YXG-158 can be used in prostate cancer-related research[1].
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YXG-158 | YXG‑158 is an orally active, anticancer bifunctional steroid analog with both androgen receptor (AR) degradation activity (DC50 = 1.28 μM) and CYP17A1 inhibitory activity (IC50 = 100 nM). YXG-158 reduces AR protein and mRNA expression via proteasome-dependent degradation, degrades AR-V7, and inhibits CYP17A1 enzymatic activity to block androgen biosynthesis. YXG-158 inhibits the activities of ERα and ERβ, as well as cancer cell proliferation. YXG-158 decreases the weight of androgen-sensitive organs in castrated rats treated with testosterone propionate, downregulates AR protein, reduces PSA levels, and suppresses tumor growth in Enzalutamide (HY-70002)-sensitive and -resistant xenograft models. YXG-158 can be used in prostate cancer-related research. | |||||||||||||||||||||
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