Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T80633 | Androgen receptor degrader-1 | Androgen Receptor | Endocrinology/Hormones |
Androgen receptor degrader-1 (compound 18)作为高效的雄激素受体降解剂, 主要应用于癌症研究。 | |||
T13273 |
UT-34
|
Androgen Receptor | Endocrinology/Hormones |
UT-34 是选择性的、具有口服活性的泛雄激素受体拮抗剂和降解剂,能够作用于野生型 AR (IC50:211.7 nM)、F876L-AR (IC50:262.4 nM)、W741L-AR (IC50:215.7 nM)。它与配体结合结构域和功能 1结构域结合,并需要泛素蛋白酶体途径来降解AR。它有抗前列腺癌的能力。 | |||
T80647 | Androgen receptor degrader-2 | Androgen Receptor | Endocrinology/Hormones |
Androgen Receptordegrader-2 (compound 9) 为有效雄激素受体降解剂,适用于癌症研究。 | |||
T79891 |
Androgen receptor degrader-3
|
Androgen Receptor | Endocrinology/Hormones |
Androgen receptordegrader-3是选择性雄激素受体降解剂,具有阻断雄激素受体信号传导并降解受体本体的能力,适用于前列腺癌疾病研究。 | |||
T18596 |
PROTAC AR Degrader-4
|
Others | Others |
PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1]. | |||
T74520 |
TD-802
|
||
TD-802 (Compound 33c) 是一种雄激素受体 (androgen receptor)PROTAC 降解剂。TD-802 具有良好的体内抗肿瘤效果,能被用于转移性去势抵抗性前列腺癌的研究。 | |||
T18873 |
VHL Ligand-Linker Conjugates 17
|
Others | Others |
VHL Ligand-Linker Conjugates 17 are chemical compounds that consist of a VHL ligand specialized for the E3 ubiquitin ligase, as well as a PROTAC linker. These conjugates are utilized in the synthesis of various PROTACs, including the notable ARD-266. ARD-266 is an exceptionally effective androgen receptor (AR) PROTAC degrader[1]. | |||
T73726 | PROTAC AR Degrader-4 TFA | ||
PROTACAR Degrader-4 包含IAP 配体结合基团,linker 和雄激素受体 (AR) 配体结合基团。基于cIAP1的降解剂也被称为SNIPER。 | |||
T13552 |
ARD-266
|
Others | Others |
ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces the degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines (DC50s: 0.2-1 nM). | |||
T14318 |
ARCC-4
|
Others | Others |
ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide and it is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy[1]. | |||
T74410 | PROTAC AR-V7 degrader-1 | ||
PROTACAR-V7 degrader-1 (Compound 6)为一种口服有效的,选择性针对AR-V7的降解剂,DC50值为0.32 µM,其作用机制主要是通过VHL E3连接酶将其招募至雄激素受体DNA结合域(AR DBD)。此外,PROTACAR-V7 degrader-1在表达AR-V7的22Rv1细胞系中展现出了活性,EC50值为0.88 µM。 | |||
T74745 |
A031
|
||
A031 是一种高效的 PROTAC 雄激素受体 (AR) 降解剂,对 AR 蛋白具有降解作用,IC50值小于 0.25 μM。A031 抑制移植人前列腺癌 (VCaP) 的斑马鱼的肿瘤生长。 | |||
T78922 |
ARD-2051
|
PROTACs | PROTAC |
ARD-2051是一种具有口服活性的高效雄激素受体(AR)蛋白水解靶向嵌合体降解剂。在LNCaP和VCaP前列腺癌细胞系中,ARD-2051实现AR蛋白降解的DC50值仅为0.6 nM,适用于前列腺癌研究。 | |||
T79725 |
ARD-1676
|
Androgen Receptor | Endocrinology/Hormones |
ARD-1676为口服有效的雄激素受体(AR) PROTAC降解剂,结合了AR配体与cereblon配体。该化合物能降解体内外的AR,并在小鼠异种移植VCaP肿瘤模型中显示抑制肿瘤生长的活性。 | |||
T13958 | VHL Ligand 8 | Others | Others |
VHL Ligand 8 是一种 von Hippel-Lindau (VHL) 蛋白配体,可用于合成 ARD-266 。ARD-266 是一种基于 VHL E3 连接酶的高效雄激素受体 (AR) PROTAC 降解剂。ARD-266 在 AR 阳性 LNCaP,VCaP 和 22Rv1 前列腺癌细胞系中有效诱导 AR 蛋白降解,DC50值为 0.2-1 nM。 | |||
T79519 |
YXG-158
|
Androgen Receptor | Endocrinology/Hormones |
YXG-158(Compound 23-h)是具有口服活性的AR降解剂和CYP17A1抑制剂。该化合物的AR降解活性表现在其DC50值为1.28 μM,而对CYP17A1的抑制作用则体现在其IC50值为100 nM。YXG-158适用于研究恩杂鲁胺耐药性前列腺癌。 |