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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6889 |
MI-136
|
Apoptosis; Epigenetic Reader Domain; Androgen Receptor | Apoptosis; Chromatin/Epigenetic; Endocrinology/Hormones |
MI136 是 menin-MLL(PPI) 蛋白互作的抑制剂,其 IC50值为31 nM,Kd 值为23.6 nM。它可抑制 DHT 诱导的雄激素受体 (AR) 靶基因的表达,有用于去势抵抗性肿瘤的潜能。 | |||
T9246 |
JNJ-63576253
|
Androgen Receptor | Endocrinology/Hormones |
JNJ63576253 是具有口服活性的、有效的雄激素受体的完全拮抗剂,在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的IC50值分别为 37 和 54 nM。它可用于研究去势抵抗性前列腺癌。 | |||
T6258 |
Zibotentan
ZD4054 |
Apoptosis; Endothelin Receptor | Apoptosis; GPCR/G Protein |
Zibotentan (ZD4054) 是一种选择性的,具有口服活性的内皮素 A (ETA) 受体拮抗剂,Ki 为 13 nM。它具有抗癌作用,可研究去势抵抗性前列腺癌。 | |||
T38684 |
AKR1C3-IN-4
AKR1C3-IN-4 |
NADPH | Metabolism |
AKR1C3-IN-4 是醛酮还原酶 1C3 (AKR1C3) 选择性抑制剂,IC50为 0.56 μM。它在去势抵抗性前列腺癌中有研究的价值。 | |||
T36841 |
IPI-9119
|
Fatty Acid Synthase | Metabolism |
IPI-9119 是一种具有口服活性、选择性和不可逆的 FASN 抑制剂 (IC50 = 0.3 nM)。 | |||
T9446 |
KB-0742 dihydrochloride
|
CDK | Cell Cycle/Checkpoint |
KB-0742 dihydrochloride 是一种有效的、选择性的、口服的 CDK9 抑制剂,具有抗肿瘤活性,对CDK9/cyclin T1的IC50为 6 nM。它对CDK9/cyclin T1具有选择性,其选择性是其他 CDK 激酶的 50 倍以上。 | |||
T8933 |
JNJ-63576253 free base
TRC253,JNJ-63576253 |
Androgen Receptor | Endocrinology/Hormones |
JNJ-63576253 free base (TRC253) 是具有口服活性的、有效的雄激素受体的完全拮抗剂,在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的 IC50值分别为 37 和 54 nM。它可用于研究去势抵抗性前列腺癌 (CRPC) 。 | |||
T76758 |
Rilotumumab
AMG 102 |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
Rilotumumab (AMG 102) 是一种针对肝细胞生长因子的单克隆抗体,对 HGF/MET 驱动的信号传导有抑制作用。Rilotumumab 具有抗肿瘤作用,可用于研究去势抵抗性前列腺癌 (CRPC) 和胃癌。 | |||
T28502 |
Ralaniten
EPI-002 |
Androgen Receptor | Endocrinology/Hormones |
Ralaniten (EPI-002) 是一种具有有效性、特异性和口服活性的雄激素受体 N 端结构域 (AR-NTD) 拮抗剂。Ralaniten 对 AR 转录活性有抑制作用,IC50 值为 7.4 μM。Ralanites 具有抗癌活性,可用于研究去势抵抗性前列腺癌 (CRPC) 。 | |||
T39954 |
AU-15330
|
Epigenetic Reader Domain; PROTACs | Chromatin/Epigenetic; PROTAC |
AU-15330是SWI/SNF ATPase亚基SMARCA2和SMARCA4的蛋白水解靶向嵌合体(PROTAC)降解剂。AU-15330 能有效抑制肿瘤在前列腺癌异种移植模型中的生长,并与 AR 拮抗剂恩杂鲁胺具有协同作用。AU-15330在去势抵抗性前列腺癌(CRPC)模型中显示出部分治疗效果和AU-15330具有无毒性的特点。 | |||
T16807 |
Rucaparib monocamsylate
瑞卡帕布樟脑磺酸盐,Rucaparib Camsylate |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rucaparib monocamsylate (Rucaparib Camsylate) 是一种口服有效的 PARP 蛋白抑制剂,对 PARP-1 的Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。 | |||
T7752 |
(S,R,S)-AHPC-Me
VHL ligand 2,E3 ligase Ligand 1A |
Ligand for E3 Ligase | PROTAC |
(S,R,S)-AHPC-Me (E3 ligase Ligand 1A) 是基于 (S,R,S)-AHPC 的的 VHL 配体,可用于募集 von Hippel-Lindau (VHL) 蛋白。它可有效降解去势抵抗性前列腺癌细胞中的 BET 蛋白,DC50<1 nM。它可用于合成 ARV-771。 | |||
T9005 |
VPC-80051 racemate
|
Others | Others |
VPC-80051 是一种有效的 hnRNP A1 剪接活性抑制剂,靶向 hnRNP A1 RBD 并降低 22Rv1 CRPC 细胞系中的 AR-V7 信使水平。 | |||
T4463 |
Rucaparib
AG-14447,PF-01367338,瑞卡帕布,AG014699 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rucaparib (PF-01367338) 是一种口服有效的 PARP 蛋白抑制剂,对 PARP-1 的 Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。 | |||
T6127 |
Rucaparib Phosphate
AG-014699 phosphate,PF-01367338,芦卡帕利,AG-014699,瑞卡帕布磷酸盐,PF-01367338 phosphate |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Rucaparib Phosphate (PF-01367338 phosphate) 是一种口服有效的PARP 蛋白抑制剂,对 PARP-1 的Ki 为 1.4 nM。它是六磷酸己糖脱氢酶 (H6PD) 抑制剂,有用于去势抵抗性前列腺癌 (CRPC) 的研究潜力。 | |||
T74094 |
5,6-Dihydroabiraterone
|
||
5,6-Dihydroabiraterone 是 Abiraterone 的代谢物。Abiraterone 是一种强效且不可逆的 CYP17A1抑制剂,具有抗雄激素活性,并在 CRPC (去势抵抗性前列腺癌) 中显示出抗肿瘤活性。 | |||
T63065 |
Rucaparib tartrate
|
||
Rucaparib (AG014699) tartrate 是一种口服具有活力的 PARP 蛋白 (PARP-1, PARP-2 和 PARP-3) 抑制剂,作用于 PARP-1 (Ki: 1.4 nM)。Rucaparib tartrate 是一种六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib tartrate 具有潜力用于去势抵抗性前列腺癌 (CRPC) 的研究。 | |||
T63811 |
EPI-7170
|
||
EPI-7170 是一种 ralaniten 类似物,是雄激素受体 N 端结构域 (androgen receptor N-terminal structural domain) 的有效拮抗剂,能够阻断全长 AR (FL-AR) 和 AR 剪接变体 (AR-Vs) 的转录活性。 EPI-7170 对 enzalutamide 耐药的去势抵抗性前列腺癌 (CRPC) 表现出抗肿瘤活性。 | |||
T61653 | VPC-13789 | ||
VPC-13789 is a highly potent, selective, and orally bioavailable antiandrogen compound that shows promise for studying and developing therapeutics for castration-resistant prostate cancer (CRPC). In LNCaP cells, VPC-13789 effectively inhibits the transcriptional activity of the androgen receptor (AR) with an IC50 value of 0.19 μM [1]. | |||
T64289 | Rucaparib camsylate | ||
Rucaparib (AG014699) camsylate 是一种口服具有活力的 PARP 蛋白 (PARP-1、PARP-2 及 PARP-3) 抑制剂,对 PARP-1 的 Ki=1.4 nM。Rucaparib camsylate 是一种六磷酸己糖脱氢酶 (H6PD) 抑制剂。Rucaparib camsylate 具有潜力进行去势抵抗性前列腺癌 (CRPC) 的研究研究。 | |||
T70847 |
BMS-351
|
||
BMS-351 is a potent and selective, nonsteroidal CYP17A1 lyase inhibitor with robust selectivity over steroidogenic CYPs 21A2 and 11B1. BMS-351 emerges as an outstanding preclinical candidate to treat CRPC and is likely to minimize the side effects of current therapies due to its exceptional selectivity. BMS-351 is potentially useful for the Treatment of Prostate Cancer. | |||
T61335 |
Rucaparib hydrochloride
|
||
Rucaparib hydrochloride, also known as AG014699, is a powerful and orally active compound that inhibits PARP proteins including PARP-1, PARP-2, and PARP-3 with a Ki value of 1.4 nM for PARP1. Additionally, Rucaparib hydrochloride acts as a modest inhibitor of hexose-6-phosphate dehydrogenase (H6PD). This compound shows potential in research for castration-resistant prostate cancer (CRPC) [1] [2] [3] [4]. | |||
T61657 | Rucaparib acetate | ||
Rucaparib (AG014699) acetate is a highly effective oral inhibitor of PARP proteins, specifically targeting PARP-1, PARP-2, and PARP-3, with a Ki value of 1.4 nM for PARP1. Additionally, it exhibits inhibitory action on hexose-6-phosphate dehydrogenase (H6PD) to a moderate extent. Rucaparib acetate shows promise in the field of research for castration-resistant prostate cancer (CRPC). [1] [2] [3] [4] | |||
T13671L |
(S,R,S)-AHPC-Me dihydrochloride
VHL ligand 2 dihydrochloride,E3 ligase Ligand 1 dihydrochloride,(S,R,S)-AHPC-Me dihydrochloride (1948273-02-6 free base) |
Others | Others |
(S,R,S)-AHPC-Me dihydrochloride, also known as VHL ligand 2 dihydrochloride, is a chemical compound utilized in the synthesis of ARV-771. ARV-771, a BET PROTAC degrader relying on von Hippel-Landau (VHL) E3 ligase, demonstrates potent degradation of BET protein in castration-resistant prostate cancer (CRPC) cells, with a DC50 of less than 1 nM. This compound serves as the VHL ligand, specifically the (S,R,S)-AHPC-based VHL ligand, that facilitates the recruitment of von Hippel-Lindau (VHL) prote... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2895 |
Lupeol
Fagarasterol,羽扇豆醇,Monogynol B,Clerodol,(3β,13ξ)-Lup-20(29)-en-3-ol,Farganasterol |
Apoptosis; Androgen Receptor; Akt | Apoptosis; Cytoskeletal Signaling; Endocrinology/Hormones; PI3K/Akt/mTOR signaling |
Lupeol (Monogynol B) 是一个活跃的五环三萜,具有抗氧化剂、抗肿瘤和抗炎活性。它是一种雄激素受体抑制剂,可研究癌症,特别是雄激素依赖表型和去势抵抗表型的前列腺癌。 | |||
T82326 | Genkwadaphnin | ||
Genkwadaphnin是一种瑞香烷二萜,能够靶向内输蛋白importin-β1,减少CRPC核心驱动因子在细胞核内的积累,并关闭其下游致癌信号通路。此外,Genkwadaphnin在小鼠体内显现出能显著抑制去势抵抗性前列腺癌(CRPC)发展的抗癌活性。 | |||
T39071 | Thailanstatin D | ||
Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis. |