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Search Results for " prostate tumor "

41

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T39695	ARD-2128	Androgen Receptor	Endocrinology/Hormones
	ARD-2128 是高效的雄激素受体降解剂 PROTAC。它可有效降低雄激素受体蛋白并抑制肿瘤组织中雄激素受体调节的基因，在没有毒性迹象的情况下抑制肿瘤生长。它有用于前列腺癌研究的价值。
T6400	AZD3514	Androgen Receptor	Endocrinology/Hormones
	AZD3514 是一种口服雄激素受体下调剂(Ki :2.2 μM)，能够减少 AR 蛋白表达。
T20681	Estramustine NSC-89201,NSC 89201,LEO 275,LEO275,雌莫司汀,NSC89201,LEO-275	Microtubule Associated	Cytoskeletal Signaling
	Estramustine (LEO-275) 是一种与雌二醇相连的氮芥，通常为磷酸盐。它已被用于治疗前列腺肿瘤；还具有防辐射功能。它被前列腺细胞选择性吸收，并通过干扰微管动力学和降低血浆睾酮水平发挥抗肿瘤作用。
T71534L	CIA-1 (Free base) CIA-1(Free base）	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	CIA-1 (Free base) 是一种核受体 COUP-TFII 抑制剂，在前列腺癌细胞系中IC50 值在 1.2 μM 到 7.6 μM 之间。CIA-1 (Free base) 在前列腺癌异种移植小鼠模型中抑制肿瘤生长。
T17228	Sabizabulin ABI-231,VERU-111	Microtubule Associated	Cytoskeletal Signaling
	Sabizabulin (ABI-231) 是一种有效且具有口服生物利用度的 α 和 β 微管蛋白抑制剂，可对抗黑色素瘤和前列腺癌细胞系。 Sabizabulin 通过靶向 HPV E6 和 E7 抑制宫颈癌细胞的肿瘤生长和转移表型。 Sabizabulin 显示出抗增殖活性，可用于前列腺癌研究。
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。
T60248	4-Aminobenzamidine dihydrochloride p-Aminobenzamidine dihydrochloride	Serine Protease	Proteases/Proteasome
	4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) 是一种强胰蛋白酶 (trypsin)抑制剂，也是一种相对较弱的尿激酶型纤溶酶原激活剂 (uPA) 抑制剂 (Ki=82 μM)。4-Aminobenzamidine 可抑制 SCID 小鼠体内前列腺肿瘤的生长。
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。
T60372	ALDH3A1-IN-1
	ALDH3A1-IN-1 (Compound 18) 是一种有效的ALDH3A1抑制剂，IC50为 1.61 μM。ALDH3A1-IN-1 比 DEAB 更有效地对抗患者来源的原发性前列腺肿瘤上皮细胞，无论是作为单药或与多西紫杉醇联合治疗。
T15594	MKC8866	IRE1	Cell Cycle/Checkpoint
	MKC8866 是一种选择性IRE1 RNase 抑制剂，在体外的IC50为 0.29 μM，是水杨醛类似物。它抑制乳腺癌细胞中的 IRE1 RNase，导致促肿瘤因子的产生减少，并且可以抑制前列腺癌 (PCa) 肿瘤的生长。它强烈抑制二硫苏糖醇诱导的 XBP1s 表达，EC50为 0.52 μM。
T71703L	Isomer-Turosteride Isomer-Turosteride(Isomer-137099-09-3)	Reductase	Endocrinology/Hormones; Metabolism
	Isomer-Turosteride (Isomer-Turosteride(Isomer-137099-09-3)) 是一种新型 5α- 还原酶抑制剂。Isomer-Turosteride 在成年大鼠中的抗前列腺作用与抑制T向 DHT 的转化有关。Isomer-Turosteride引起前列腺 DHT 的降低，与 T 含量的继发性增加无关。Isomer-Turosteride 具有抗癌活性，可抑制肿瘤细胞的生长。
T25294	DCFBC F-18 18F-DCFBC
	DCFBC F-18 is a radioconjugate containing a low molecular weight tracer, DCFBC, specific for prostate-specific membrane antigen (PSMA) and labeled with the positron-emitting isotope F 18 with potential prostate tumor imaging upon positron emission tomogra
T28203	NSC156529 NSC-156529,NSC 156529
	NSC156529 downregulates AKT1 signaling. NSC156529 efficiently decreases the proliferation of human cancer cells in vitro, and substantially inhibits the growth of prostate tumor xenografts in vivo.
T69479	CGC 11093
	CGC 11093 is a polyamine analog; inhibits growth of human prostate tumor xenografts in nude mice. It may prove useful in promoting regression of choroidal neovascularization.
T71494	ISC-4
	ISC-4 is an Akt inhibitor, which activates prostate apoptosis response protein-4 and reduces colon tumor growth in a nude mouse model.
T41070	LP-184
	LP-184 (Compound 6), referred to as an acylfulvene analog, demonstrates the ability to inhibit tumor growth with noteworthy anti-cancer efficacy observed across multiple cell lines, including ovarian, colon, prostate, and pancreatic.
T78412	Biotin-NH-PSMA-617
	Biotin-NH-PSMA-617为标记有生物素的PSMA-617小分子，专门针对前列腺特异性膜抗原（PSMA），后者为肿瘤细胞所特有表达。
T71534	CIA-1 hcl(452087-38-6 Free base)	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	CIA-1对核受体COUP-TFII 具有抑制作用，在前列腺癌细胞系中IC50范围从1.2μM 到7.6μM 之间。CIA-1在体外抑制多种前列腺癌细胞系的生长并抑制COUP-TFII 活性以调节其靶基因。CIA-1在体内对前列腺癌异种移植小鼠模型中的肿瘤生长具有抑制作用。
T80966	Topsalysin PRX-302
	Topsalysin为PSA激活的前体蛋白质，同时是与人前列腺特异性抗原融合的孔隙形成蛋白（合成原气溶素）。研究显示Topsalysin能够抑制小鼠模型中的肿瘤生长。
T35940	Darinaparsin Dimethylarsinic glutathione,Darinaparsin
	Darinaparsin is a dimethylated arsenic linked to glutathione. It is cytotoxic to DU145, LNCaP, and PC3 prostate cancer cells (IC50s = 5-10 &#181M) and patient-derived primary prostate cancer cells (IC50s = 2.5-20 &#181M), as well as Jurkat T cell lymphoma and L540 Hodgkin lymphoma cells (IC50s = 2.7 and 1.3 &#181M, respectively). [1][2] It decreases the tumor-initiating subpopulation in DU145 and PC3 cells and halts the cell cycle in the G2/M phase. Darinaparsin decreases transcription of Gli-2,...
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...
T69758	Flutamide-d7
	Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist and prodrug form of 2-hydroxy flutamide. Flutamide is converted to 2-hydroxy flutamide by the cytochrome P450 (CYP) isoform CYP1A2 in human liver microsomes. It is cytotoxic to PC3 and LNCaP prostate cancer cells with IC50 values of 98.8 and 81.8 µM, respectively. Flutamide (50 mg/kg per day) reduces tumor growth in a PC-82 mouse xenograft mo...
T41175	OB 24 hydrochloride
	OB 24 hydrochloride is a potent and selective heme oxygenase 1 (HO-1) inhibitor (IC50 values are 1.9 and >100 μM for HO-1 and HO-2 respectively), reduces protein carbonylation and reactive oxygen species formation in advanced prostate cancer cells (PCA). Inhibits cell proliferationin vitroand PCA tumor growth and lymph node/lung metastasesin vivo. Synergizes with Taxol.
T68400	STA-9584
	STA-9584 is a potent vascular disrupting agent, which exhibits potent antitumor activity by selectively targeting microvasculature at both the center and periphery of tumors. In vitro, 2-methoxy-5-(5-(3,4,5-trimethoxyphenyl)isoxazol-4-yl)aniline (STA-9122) (active metabolite of STA-9584 ) displayed increased potency relative to other tubulin-binding agents and was highly cytotoxic to tumor cells. STA-9584 induced significant tumor regressions in prostate and breast xenograft models in vivo and, ...
T72785	PRMT5:MEP50 PPI
	PRMT5:MEP50 PPI是一款新型的抑制剂，专门针对PRMT5:MEP50蛋白-蛋白相互作用，展现了抗肿瘤活性，并对肺癌及前列腺癌细胞具有显著的抗增殖效果。
T70222	Ethonafide
	Ethonafide is an anthracene-containing derivative of amonafide that belongs to the azonafide series of anticancer agents. The lack of cross-resistance in multidrug-resistant cancer cell lines and the absence of a quinone and hydroquinone moiety make ethonafide a potentially less cardiotoxic replacement for existing anthracene-containing anticancer agents. Ethonafide was cytotoxic against three human prostate cancer cell lines at nanomolar concentrations. Ethonafide was found to be better tolerat...
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。
T36991	Monascuspiloin
	Monascuspiloin is a fungal metabolite that has been found inM. pilosusM93-fermented rice.1It induces endoplasmic reticulum stress and autophagy in PC3 prostate cancer cells. Monascuspiloin (15-45 μM) decreases viability of PC3 cells and has an additive effect on the reduction in viability of PC3 cells induced by irradiation when used at a concentration of 25 μM. It induces intratumor apoptosis and autophagy and reduces tumor growth in a PC3 mouse xenograft model when administered at doses of 40 ...
T79668	PIK5-12d	Autophagy	Autophagy
	PIK5-12d为一种高效的PROTAC PIKfyve降解剂，具有显著的DC50值为1.48 nM。该化合物在多种前列腺癌细胞系中有效诱导细胞质空泡化，同时阻碍自噬流的进行，有效抑制前列腺癌细胞的增殖，并展现出抗肿瘤活性。
T60275	ALDH3A1-IN-2
	ALDH3A1-IN-2 (Compound 19) 作为一种高效的ALDH3A1抑制剂，其IC50值达到1.29 μM。由于醛脱氢酶 (ALDH) 在前列腺癌等多种肿瘤类型中的过表达，ALDH3A1-IN-2 显示出其在癌症疾病研究中的应用潜力。
T61935	B-Raf IN 9
	B-Raf IN 9 (compound 8b) 是有效的B-Raf 抑制剂（IC50= 24.79 nM）。B-Raf IN 9 将细胞周期阻滞于 G2/M 期，诱导凋亡。B-Raf IN 9 对人前列腺癌 PC-3 细胞表现出较强的抗肿瘤活性（IC50= 7.83 μM）。
T73125	SMTIN-T140	HSP	Cytoskeletal Signaling; Metabolism
	SMTIN-T140（化合物6a）是一种TRAP1（肿瘤坏死因子受体相关蛋白1）的高效抑制剂，IC50值为1.646 μM。该化合物表现出显著的抗癌活性，可引起线粒体功能障碍，增加线粒体ROS产生以及激活AMPK。在PC3前列腺癌细胞异种移植的小鼠模型中，SMTIN-T140有效抑制了肿瘤生长，并显示出良好的体内安全性。
TMIH-0089	Androstenedione-d7
	Androstenedione-d7 是 Androstenedione 的氘代化合物。Androstenedione 的 CAS 号为 560-62-3。9-hydroxy-4-androstene-3,17-dione 是一种类固醇激素，具有抗肿瘤活性，可以抑制多种癌症细胞的生长，包括乳腺癌、前列腺癌和肺癌细胞。
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 ...
T71252	PC-046
	PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with di...
T68401	IG-105
	IG-105 is a potent microtubule inhibitor with potential anticancer activity. IG-105 inhibits microtubule assembly by binding at colchicine pocket. IG-105 shows a potent anticancer activity in vitro and in vivo and has good safety in mice. IG-105 showed a potent activity against human leukemia and solid tumors in breast, liver, prostate, lung, skin, colon, and pancreas with IC(50) values between 0.012 and 0.298 mumol/L. It was also active in drug-resistant tumor cells and not a P-glycoprotein sub...
T36195	CAY10744
	CAY10744 is a topoisomerase II-α poison.1 It inhibits topoisomerase II-α by 78.9% when used at a concentration of 20 μM. CAY10744 is selective for topoisomerase II-α over topoisomerase I providing 100 and 0% inhibition, respectively, at 100 μM. It inhibits proliferation of HCT15 colon, T47D breast, DU145 prostate, and HeLa cervical cancer cells (IC50s = 0.014, 0.00267, 0.072, and 2.46 μM, respectively). CAY10744 induces apoptosis in T47D cells when used at concentrations of 10 and 30 μM. CAY1074...
T60737	LG308
	LG308 是一种新型合成化合物，具有抗微管活性。LG308 诱导细胞凋亡和细胞死亡，并且显著抑制肿瘤生长，具有前列腺癌的研究潜力。LG308 诱导有丝分裂阻滞并显着抑制 G2/M 的进程，这与细胞周期蛋白 B1 和有丝分裂标志物 MPM-2 的上调以及 cdc2 的去磷酸化有关。
T75142	Acid Ceramidase-IN-2
	Acid Ceramidase-IN-2（compound 1）是一款针对酸性神经酰胺酶（ceramidase）的抑制剂，显示出抗增殖及细胞活性抑制的潜力。有研究表明，该化合物在前列腺癌细胞中可阻止人酸性神经酰胺酶的过度表达，从而揭示了其潜在的抗肿瘤能力。此外，Acid Ceramidase-IN-2被三种α-酮酰胺：GT85、GT98和GT99在体外有效抑制其水解作用。
T36085	PKI-179 hydrochloride
	PKI-179 is an orally bioavailable dual inhibitor of PI3K and mammalian target of rapamycin (mTOR). In an in vitro enzymatic assay, it potently inhibits PI3K (IC50s = 8, 24, 17, and 74 nM for isoforms α, β, δ, and γ, respectively), two common PI3Kα mutants, E545K and H1047R (IC50s = 14 and 11 nM, respectively), and mTOR (IC50 = 0.42 nM). PKI-179 is selective for PI3K and mTOR over a panel of 361 other kinases at IC50 values up to 50 μM, hERG (IC50 > 30 μM), and cytochrome P450 (CYP) isoforms (IC5...
T78810	BWA-522	Androgen Receptor	Endocrinology/Hormones
	BWA-522是一种口服有效的小分子PROTACs，针对AR-FL和AR-V7显示出显著的降解活性。该化合物通过对Androgen Receptor的AR-NTD进行拮抗，诱发PC细胞的apoptosis。在LNCaP异种移植模型中，BWA-522以每日60 mg/kg的剂量口服给药，实现了76%的肿瘤生长抑制(TGI=76%)。在VCaP和LNCaP细胞系中对AR-V7和AR-FL的降解效率分别达到77.3%(1 μM)和72.0%(5 μM)。

化合物

Cat.No: T39695

Target: Androgen Receptor

Cat.No: T6400

Target: Androgen Receptor

Cat.No: T20681

Synonym: NSC-89201,NSC 89201,LEO 275,LEO275,雌莫司汀,NSC89201,LEO-275

Target: Microtubule Associated

CIA-1 (Free base)

Cat.No: T71534L

Synonym: CIA-1(Free base）

Target: Gamma-secretase

Cat.No: T17228

Synonym: ABI-231,VERU-111

Target: Microtubule Associated

Cat.No: T39954

Target: Epigenetic Reader Domain, PROTACs

4-Aminobenzamidine dihydrochloride

Cat.No: T60248

Synonym: p-Aminobenzamidine dihydrochloride

Target: Serine Protease

Cat.No: T76743

Synonym: LY2875358

Target: c-Met/HGFR

Cat.No: T60372

Cat.No: T15594

Target: IRE1

Isomer-Turosteride

Cat.No: T71703L

Synonym: Isomer-Turosteride(Isomer-137099-09-3)

Target: Reductase

Cat.No: T25294

Synonym: 18F-DCFBC

Cat.No: T28203

Synonym: NSC-156529,NSC 156529

Cat.No: T69479

Cat.No: T71494

Cat.No: T41070

Biotin-NH-PSMA-617

Cat.No: T78412

CIA-1 hcl(452087-38-6 Free base)

Cat.No: T71534

Target: Gamma-secretase

Cat.No: T80966

Synonym: PRX-302

Cat.No: T35940

Synonym: Dimethylarsinic glutathione,Darinaparsin

Minnelide free acid

Cat.No: T71113

Cat.No: T69758

OB 24 hydrochloride

Cat.No: T41175

Cat.No: T68400

PRMT5:MEP50 PPI

Cat.No: T72785

Cat.No: T70222

Cat.No: T74745

Cat.No: T36991

Cat.No: T79668

Target: Autophagy

Cat.No: T60275

Cat.No: T61935

Cat.No: T73125

Target: HSP

Androstenedione-d7

Cat.No: TMIH-0089

Histone H3K27Me1 (23-34) (trifluoroacetate salt)

Cat.No: T36980

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

Cat.No: T71252

Cat.No: T68401

Cat.No: T36195

Cat.No: T60737

Acid Ceramidase-IN-2

Cat.No: T75142

PKI-179 hydrochloride

Cat.No: T36085

Cat.No: T78810

Target: Androgen Receptor

Cat. No.	Product Name	Target	Signaling Pathways
T3324	Lycorine Galanthidine,Narcissine,石蒜碱,Amarylline,Belamarine,Licorine,番石榴碱	Apoptosis; Virus Protease; Antibacterial; AChR; Fatty Acid Synthase	Apoptosis; Metabolism; Microbiology/Virology; Neuroscience
	Lycorine (Narcissine) 是从金眼科植物科中提取的一种天然生物碱。它是一种具有口服活性的SCAP 抑制剂，Kd 值 15.24 nM。它也是黑色素瘤血管生成抑制剂，有用于前列腺癌和代谢疾病的研究潜力。
T6290	Tanespimycin 坦螺旋霉素,17-AAG,CP 127374,NSC 330507,KOS 953	Apoptosis; Mitophagy; HSP; Antibacterial; Antibiotic; Autophagy	Apoptosis; Autophagy; Cytoskeletal Signaling; Metabolism; Microbiology/Virology
	Tanespimycin (KOS 953) 是一种 Hsp90 抑制剂，可选择性抑制 BT474 肿瘤细胞 Hsp90，IC50为 5 nM。它消耗细胞内 STK38/NDR1，并降低 STK38 激酶活性，还能下调stk38基因表达。
T7990	9-hydroxy-4-androstene-3,17-dione	Others	Others
	9-hydroxy-4-androstene-3,17-dione 是一种类固醇激素，具有抗肿瘤活性，可以抑制多种癌症细胞的生长，包括乳腺癌、前列腺癌和肺癌细胞。
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.
TN4774	Physalin A	ERK; BCL; p38 MAPK; NF-κB; Androgen Receptor; ROS; JAK; JNK; STAT; p53; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Endocrinology/Hormones; Immunology/Inflammation; JAK/STAT signaling; MAPK; NF-κB; Stem Cells
	Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth through activation of cell apoptosis and downregulation of androgen receptor ex
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: T3324

Synonym: Galanthidine,Narcissine,石蒜碱,Amarylline,Belamarine,Licorine,番石榴碱

Target: Apoptosis, Virus Protease, Antibacterial, AChR, Fatty Acid Synthase

Cat.No: T6290

Synonym: 坦螺旋霉素,17-AAG,CP 127374,NSC 330507,KOS 953

Target: Apoptosis, Mitophagy, HSP, Antibacterial, Antibiotic, Autophagy

9-hydroxy-4-androstene-3,17-dione

Cat.No: T7990

Target: Others

Thailanstatin D

Cat.No: T39071

Cat.No: TN4774

Target: ERK, BCL, p38 MAPK, NF-κB, Androgen Receptor, ROS, JAK, JNK, STAT, p53, Autophagy

Cat.No: T82326

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