32
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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8217 |
Enzalutamide carboxylic acid
|
Androgen Receptor; Drug Metabolite | Endocrinology/Hormones; Metabolism |
Enzalutamide carboxylic acid 是 Enzalutamide 非活性代谢物。Enzalutamide 是雄激素受体 (AR) 拮抗剂。 | |||
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。 | |||
T22263 |
Bavdegalutamide
ARV-110 |
Androgen Receptor | Endocrinology/Hormones |
Bavdegalutamide (ARV-110) 是一种雄激素受体 (AR) 的 PROTAC 降解剂。 Bavdegalutamide 可用于前列腺癌的研究。 Bavdegalutamide 具有口服活性和选择性,并促进 AR 的泛素化和降解。 | |||
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。 | |||
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)。 | |||
T0380 |
Bicalutamide
比卡鲁胺,ICI-176334 |
Androgen Receptor; Autophagy | Autophagy; Endocrinology/Hormones |
Bicalutamide (ICI-176334) 是一种具有口服活性的非甾体雄激素受体拮抗剂,可研究前列腺癌。 | |||
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) 。 | |||
T8497 |
SX-682
|
CXCR | Autophagy; GPCR/G Protein; Immunology/Inflammation |
SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂,可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫,具有治疗去势抵抗性前列腺癌的潜力。 | |||
T6215 |
Abiraterone Acetate
Zytiga,乙酸阿比特龙酯,CB7630 |
P450 | Metabolism |
Abiraterone Acetate (CB7630) 是一种具有口服活性的、不可逆的 CYP17A1选择性抑制剂,具有抗雄激素作用。它是 Abiraterone 的前药。 | |||
T13363 |
Y06137
|
Epigenetic Reader Domain; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
Y06137 是一种有效的特异性 BET 抑制剂,对 BRD4(1) 溴结构域的 Kd 为 81 nM。 Y06137可用于去势抵抗性前列腺癌治疗的研究。 | |||
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。 | |||
T13671 |
(S,R,S)-AHPC-Me hydrochloride
VHL ligand 2 hydrochloride,E3 ligase Ligand 1 |
Others; Ligand for E3 Ligase | Others; PROTAC |
(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a chemical compound utilized in the synthesis of ARV-771, an exceptionally potent BET protein degrader. This compound selectively degrades BET protein in cells resistant to castration, exhibiting a remarkable DC50 <1 nM. Recognized as VHL ligand 2 hydrochloride, (S,R,S)-AHPC-Me hydrochloride serves as the VHL ligand derived from (S,R,S)-AHPC for the recruitment of von Hippel-Lindau (VHL) protein. | |||
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。 | |||
T76743 |
Emibetuzumab
LY2875358 |
c-Met/HGFR | Tyrosine Kinase/Adaptors |
Emibetuzumab 是一种有效的人源化二价 MET 抗体 (IgG4 型)。Emibetuzumab 具有抗肿瘤活性,对 HGF 依赖性和非依赖性 MET 通路的激活和肿瘤生长有抑制作用可用于研究晚期去势抵抗性前列腺癌。 | |||
T26831 |
BKM1644
BKM 1644,BKM-1644 |
||
BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells. | |||
T69874 | LLS30 | ||
LLS30 is an allosteric inhibitor of Galectin-1 (Gal-1). LLS30 decreases Gal-1 binding affinity to its binding partners, and potentially overcomes metastatic castration-resistant prostate cancer (mCRPC). | |||
T17930 |
EC1167
|
Others | Others |
EC1169 is a targeted tubulysin conjugate that utilizes EC1167 as its linker. This compound shows promise in the treatment of recurrent metastatic, castration-resistant prostate cancer (MCRPC)[1]. | |||
T61109 |
HG122
|
||
HG122 is a chemical compound that effectively facilitates the degradation of androgen receptor (AR) via the proteasome pathway, leading to the inhibition of castration-resistant prostate cancer. | |||
T75058 | RLA-5331 | ||
RLA-5331,一种含有抗雄激素的铁活化剂,针对(mCRPC)细胞系显示出抗增殖活性。 | |||
T6051 |
Orteronel
TAK-700,(S)-Orteronel |
P450 | Metabolism |
(S)-Orteronel ((S)-Orteronel) 是人17,20-裂解酶 (17,20-lyase, CYP17) 选择性抑制剂(IC50:38 nM),CYP17对(S)-Orteronel 选择性比对 11-hydroxylase 及 CYP3A4 高 1000 多倍。 | |||
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]. | |||
T75057 | RLA-4842 | ||
RLA-4842,含有抗雄激素性质的铁活化剂,表现出对于转移性去势抵抗性前列腺癌(mCRPC)细胞系的抗增殖活性。 | |||
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。 | |||
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]. | |||
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。 | |||
T77815 |
EC1167 hydrochloride
|
||
EC1167 hydrochloride为EC1169的linker,后者是针对前列腺特异性膜抗原的小管溶解蛋白偶联物。EC1169 hydrochloride展现了对治疗复发性转移性去势性前列腺癌(MCRPC)的研究潜力。 | |||
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] | |||
T77130 | Pasotuxizumab | ||
Pasotuxizumab (BAY 2010112) 是一种 PSMA 和 CD3双特异性的 T 细胞接合剂 (BiTE)。Pasotuxizumab 可结合CD3和 PSMA,对人CD3和 PSMA 的KD 分别为 9.4 nM 和 47.0 nM。Pasotuxizumab 可用于转移性去势抵抗性前列腺癌 (mCRPC) 的研究。 | |||
T71113 | Minnelide free acid | ||
Minnelide is an effective therapy against pancreatic cancer. Minnelide Inhibits Androgen Dependent, Castration Resistant Prostate Cancer Growth by Decreasing Expression of Androgen Receptor Full Length and Splice Variants. Minnelide reduced tumor volume in multiple models of pancreatic cancer. Minnelide was a more effective drug against pancreatic cancer models. It effectively reduced tumor burden and tumor related morbidity in different unique but complementary mouse models. It reduced metastat... | |||
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... | |||
T36980 |
Histone H3K27Me1 (23-34) (trifluoroacetate salt)
Histone H3K27Me1 (23-34) (trifluoroacetate salt) |
||
Histone H3K27Me1 (23-34) is a peptide fragment of histone H3 that corresponds to amino acid residues 24-35 of the human histone H3.1 and H3.2 sequences. Monomethylation of histone H3 at lysine 27 is associated with actively transcribed genes and positively correlates with H3K36 trimethylation. Levels of H3K27Me1 are increased in tumor tissue isolated from patients with metastatic hormone-na ve and castration-resistant prostate cancer. Histone H3K27Me1 (23-34) has been used in epitope mapping of ... | |||
T77072 | Lorigerlimab | ||
Lorigerlimab (MGD019) 为一种IgG4双特异性双亲和力再靶向抗体 (DART)。该化合物通过阻断PD-1与CTLA-4来提升T细胞反应效率,目前正被应用于转移性去势抵抗性前列腺癌 (mCRPC) 研究中。 |
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。 | |||
TQ0214 |
Dimethylcurcumin
ASC-J9,二甲基姜黄素,GO-Y025 |
Androgen Receptor | Endocrinology/Hormones |
Dimethylcurcumin (ASC-J9) 是雄激素受体降解增强剂,能够有效抑制耐药性前列腺癌细胞增殖和侵袭。 | |||
T2543 |
Cabazitaxel
XRP6258,卡巴他塞,RPR-116258A,TXD 258,taxoid XRP6258 |
Microtubule Associated; Autophagy | Autophagy; Cytoskeletal Signaling |
Cabazitaxel (taxoid XRP6258) 是一种紫杉烷类的抗肿瘤剂,可用于治疗多西他赛失败后的去势抵抗性转移性前列腺癌。 | |||
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. | |||
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。 |