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Search Results for " castration "

38

抑制剂 & 化合物

5

天然产物

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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。
T21740	RD162	Androgen Receptor	Endocrinology/Hormones
	RD162 是一种与雄激素受体 (AR) 特异性结合的非甾体抗雄激素 (NSAA)。
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。
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。
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) 。
T0272	Nilutamide 尼鲁米特,RU23908	Androgen Receptor	Endocrinology/Hormones
	Nilutamide (RU23908) 是一种非甾体抗雄激素药物，有用于转移性前列腺癌的潜力。
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。
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。
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。
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。
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.
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。
T30876	CHF 2819 Ganstigmine HCl,CHF-2819,Ganstigmine hydrochloride,CHF2819
	CH-5137291 is a pure AR antagonist with AR nuclear translocation inhibition activity. It suppresses castration and prevents the growth of prostate cancer cells.
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).
T30877	CHF-1024 UNII-HPH2L3QA2F
	CH-5137291 is a pure AR antagonist with AR nuclear translocation inhibition activity. It inhibits castration and prevents the growth of prostate cancer cells.
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].
T30868	CH-5137291 CH 5137291,CH5137291
	CH-5137291 is a pure AR antagonist with AR nuclear translocation inhibition activity. It suppresses castration and prevents the growth of prostate cancer cells.
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。
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].
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。
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。
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。
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。
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...
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...
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。
T68292	GTX-758
	GTX-758, also known as Capesaris, is a n orally available, nonsteroidal selective estrogen receptor (ER) alpha agonist with potential antineoplastic activity. Upon administration of GTx-758, this agent suppresses the secretion of the gonadotropins follicle-stimulating hormone (FSH) and luteinizing hormone (LH) by the pituitary gland through feedback inhibition. In males, the inhibition of LH secretion prevents the synthesis of androgens, including testosterone, by the testes. This may result in ...

化合物

Enzalutamide carboxylic acid

Cat.No: T8217

Target: Androgen Receptor, Drug Metabolite

Cat.No: T21740

Target: Androgen Receptor

Cat.No: T6889

Target: Apoptosis, Epigenetic Reader Domain, Androgen Receptor

Cat.No: T9246

Target: Androgen Receptor

Bavdegalutamide

Cat.No: T22263

Synonym: ARV-110

Target: Androgen Receptor

Cat.No: T36841

Target: Fatty Acid Synthase

Cat.No: T0380

Synonym: 比卡鲁胺,ICI-176334

Target: Androgen Receptor, Autophagy

JNJ-63576253 free base

Cat.No: T8933

Synonym: TRC253,JNJ-63576253

Target: Androgen Receptor

Cat.No: T0272

Synonym: 尼鲁米特,RU23908

Target: Androgen Receptor

Cat.No: T8497

Target: CXCR

Cat.No: T13363

Target: Epigenetic Reader Domain, PKC

Abiraterone Acetate

Cat.No: T6215

Synonym: Zytiga,乙酸阿比特龙酯,CB7630

Target: P450

(S,R,S)-AHPC-Me

Cat.No: T7752

Synonym: VHL ligand 2,E3 ligase Ligand 1A

Target: Ligand for E3 Ligase

Cat.No: T76758

Synonym: AMG 102

Target: c-Met/HGFR

(S,R,S)-AHPC-Me hydrochloride

Cat.No: T13671

Synonym: VHL ligand 2 hydrochloride,E3 ligase Ligand 1

Target: Others, Ligand for E3 Ligase

Cat.No: T76743

Synonym: LY2875358

Target: c-Met/HGFR

Cat.No: T30876

Synonym: Ganstigmine HCl,CHF-2819,Ganstigmine hydrochloride,CHF2819

Cat.No: T26831

Synonym: BKM 1644,BKM-1644

Cat.No: T69874

Cat.No: T30877

Synonym: UNII-HPH2L3QA2F

Cat.No: T17930

Target: Others

Cat.No: T30868

Synonym: CH 5137291,CH5137291

Cat.No: T61109

Cat.No: T75058

Cat.No: T6051

Synonym: TAK-700,(S)-Orteronel

Target: P450

Rucaparib hydrochloride

Cat.No: T61335

5,6-Dihydroabiraterone

Cat.No: T74094

Cat.No: T61653

Cat.No: T75057

Cat.No: T74520

EC1167 hydrochloride

Cat.No: T77815

Cat.No: T77130

Rucaparib acetate

Cat.No: T61657

(S,R,S)-AHPC-Me dihydrochloride

Cat.No: T13671L

Synonym: VHL ligand 2 dihydrochloride,E3 ligase Ligand 1 dihydrochloride,(S,R,S)-AHPC-Me dihydrochloride (1948273-02-6 free base)

Target: Others

Minnelide free acid

Cat.No: T71113

Histone H3K27Me1 (23-34) (trifluoroacetate salt)

Cat.No: T36980

Synonym: Histone H3K27Me1 (23-34) (trifluoroacetate salt)

Cat.No: T77072

Cat.No: T68292

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。

天然产物

Cat.No: T2895

Synonym: Fagarasterol,羽扇豆醇,Monogynol B,Clerodol,(3β,13ξ)-Lup-20(29)-en-3-ol,Farganasterol

Target: Apoptosis, Androgen Receptor, Akt

Dimethylcurcumin

Cat.No: TQ0214

Synonym: ASC-J9,二甲基姜黄素,GO-Y025

Target: Androgen Receptor

Cat.No: T2543

Synonym: XRP6258,卡巴他塞,RPR-116258A,TXD 258,taxoid XRP6258

Target: Microtubule Associated, Autophagy

Thailanstatin D

Cat.No: T39071

Cat.No: T82326

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