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55

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9756	AZD-9574	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	AZD-9574 是 SSB 位点的 PARP1 特异性抑制剂。 AZD-9574 具有抗癌活性，可用于 HRD+ 乳腺癌和晚期实体恶性肿瘤的研究。
T8327	ONO-7475	Trk receptor; TAM Receptor	Tyrosine Kinase/Adaptors
	ONO-7475 是一种选择性的、有效的、具有口服活性的Axl/Mer 抑制剂。它使 AXL 过表达的EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感，抑制耐药细胞的产生和耐药性的维持。它与 Osimertinib 联合使用，具有用于 EGFR 突变非小细胞肺癌的潜力。
T26889	Borofalan(10B) L-4-Boronophenylalanine,4-10硼酸-L-苯丙氨酸	Others	Others
	Borofalan(10B) (L-4-Boronophenylalanine) 具有抗肿瘤作用，可用于研究复发性或局部晚期头颈癌。
T30190	Ataquimast	Others	Others
	Ataquimast 用于治疗晚期受体阳性乳腺癌。
T2361	LY2874455 LY 2874455,LY-2874455	VEGFR; FGFR	Angiogenesis; Tyrosine Kinase/Adaptors
	LY2874455 是pan-FGFR 抑制剂，能够抑制FGFR1 (IC50:2.8 nM)，FGFR2 (IC50:2.6 nM)，FGFR3 (IC50:6.4 nM)，FGFR4 (IC50:6 nM)。
T27259	Emitefur BOFA2,BOF A2,BOF-A2	Others	Others
	Emitefur (BOF-A 2)是一种有口服活性和有效性的 5-氟尿嘧啶衍生物，具有抗癌和抗肿瘤活性。Emitefur 可用于研究晚期胃癌、乳腺癌和代谢相关疾病。
T17216	Valspodar PSC 833	P-gp	Membrane transporter/Ion channel; Neuroscience
	Valspodar (PSC 833) 是一种特异性的 P-糖蛋白抑制剂和MDR调节剂，常被用作化学增敏剂，可用于研究晚期上皮卵巢癌。
T15390	Glufosfamide D 19575,Glucosylifosfamide mustard	Others	Others
	Glufosfamide 是一种新型噁唑磷胺化合物，具有抗癌活性，可用于研究晚期非小细胞肺癌。
T11237	Camizestrant Estrogen receptor antagonist 2	Estrogen Receptor/ERR	Endocrinology/Hormones
	Camizestrant (Estrogen receptor antagonist 2) 是一种雌激素受体拮抗剂，可用于 ER+ HER2 晚期乳腺癌的研究[1]。
T2145	Temsirolimus NSC 683864,CCI-779,西罗莫司脂化物	Apoptosis; mTOR; Autophagy	Apoptosis; Autophagy; PI3K/Akt/mTOR signaling
	Temsirolimus (CCI-779) 是一种mTOR 抑制剂，IC50值为 1.76 μM。它能激活自噬，可防止心脏功能恶化。
T40199	Tulmimetostat CPI-0209	Histone Methyltransferase	Chromatin/Epigenetic
	Tulmimetostat (CPI-0209) 是一种具有口服活性的 EZH1/EZH2 抑制剂。Tulmimetostat 有抗肿瘤活性，用于研究卵巢癌和晚期实体瘤。
T6084	Rabusertib LY2603618,IC-83	Chk; PDK; Autophagy	Autophagy; Cell Cycle/Checkpoint; PI3K/Akt/mTOR signaling
	Rabusertib (IC-83) 是一种有效的选择性的Chk1抑制剂，IC50为 7 nM。它有潜在的化学增强活性，用于各种癌症和肿瘤治疗的试验。
T68065	Enloplatin
	Enloplatin 是一种卡铂类似物，在治疗晚期卵巢癌有部分作用。
T39403	Avotaciclib BEY1107,Avotaciclib	CDK	Cell Cycle/Checkpoint
	Avotaciclib (BEY1107) 是一种有效和具有口服活性的 cyclin dependent kinase 1 (CDK1) 抑制剂。Avotaciclib 可用于研究局部晚期或转移性胰腺癌。
T2073	GSK2636771 GSK 2636771,GSK-2636771	PI3K	PI3K/Akt/mTOR signaling
	GSK2636771 是选择性的、口服有效的PI3Kβ抑制剂，Ki=0.89 nM，IC50=5.2 nM，比p110α和p110γ的选择性高900倍，比p110δ同种型的选择性高10倍。
T74698	RMC-6236	Ras	GPCR/G Protein; MAPK
	RMC-6236 是一种 RAS(ON)MULTI 抑制剂，具有抗癌活性，可用于研究晚期恶性实体瘤和结直肠癌。
T6157	Devimistat CPI-613,辛酸,CPI613,CPI 613,6,8-Bis(benzylthio)octanoic acid	Apoptosis; Dehydrogenase; Mitochondrial Metabolism	Apoptosis; Metabolism
	Devimistat (6,8-Bis(benzylthio)octanoic acid) 是一种线粒体代谢抑制剂，还是一种lipoic acid 拮抗剂，能阻断线粒体能量代谢，诱导多种癌细胞凋亡。
T8875	CD73-IN-3 EX-A4254,LY-3475070	CD73	Immunology/Inflammation
	CD73-IN-3 (LY-3475070) 是一种有效的选择性 CD73 抑制剂，IC50 为 28 nM，具有癌症的研究潜力。
T1755	LY2090314	GSK-3	PI3K/Akt/mTOR signaling; Stem Cells
	LY2090314 是GSK-3抑制剂，抑制 GSK-3α (IC50:1.5 nM) 和 GSK-3β (IC50:0.9 nM)。
T40292	Opnurasib NVP-JDQ443,JDQ-443,Opnurasib	Ras	GPCR/G Protein; MAPK
	Opnurasib (JDQ-443) 是一种可口服且具有选择性和有效性的共价 KRAS G12C 抑制剂，具有抗肿瘤活性，可用于研究晚期非小细胞肺癌。
T0078	Lapatinib GSK572016,GW572016,拉帕替尼	EGFR; Ferroptosis; Autophagy	Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Lapatinib (GW572016) 是一种 ErbB2 和 EGFR 的抑制剂 (IC50=9.2/10.8 nM)，具有口服活性。Lapatinib 具有抗肿瘤活性，可以用于治疗 HER2 过表达的晚期或转移性乳腺癌。
T2381	Abemaciclib CDK4/6 dual inhibitor,LY2835219	CDK	Cell Cycle/Checkpoint
	Abemaciclib (LY2835219) 是一种 CDK4/6 的双重抑制剂 (IC50=2/10 nM)，具有选择性和特异性。Abemaciclib 具有抗肿瘤活性，被用于治疗晚期或转移性乳腺癌。
T0078L	Lapatinib ditosylate monohydrate Lapatinib ditosylate monohydrate,Lapatinib ditoluenesulfonate monohydrate,Lapatinib tosilate hydrate,Lapatinib tosilate,Tykerb,二甲苯磺酸拉帕替尼单水合物,Tyverb	EGFR; Ferroptosis; Autophagy	Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Lapatinib ditosylate (Lapatinib tosilate) monohydrate 是一种有效的 EGFR 和 ErbB2 抑制剂，对 EGFR 和 ErbB2的 IC50值分别为 10.8 和 9.2 nM。它用于治疗晚期乳腺癌和其他实体瘤。
T6883	Samotolisib GTPL8918,LY3023414	DNA-PK; PI3K; mTOR; Autophagy	Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	Samotolisib (LY3023414) 在低纳摩尔浓度下，有效抑制mTORC1/2。它选择性地有效抑制PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ、DNA-PK 和mTOR，IC50分别为 6.07 nM、77.6 nM、38 nM、23.8 nM、4.24 nM 和 165 nM。它可用于多种肿瘤和癌症的试验。
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。
T2283	PX-12 2-[(1-甲基丙基)二硫代]-1H-咪唑,IV-2,PX12	Thioredoxin	Metabolism
	PX-12 (PX12) 是一种可逆的硫氧还蛋白-1(Trx-1)抑制剂，能够抑制 MCF-7 细胞(IC50:1.9 μM)和HT-29 细胞(IC50:2.9 μM)的生长。
T14997	Conteltinib SY-707,CT-707	FAK; PYK2; ALK	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Conteltinib (CT-707) 是一种靶向FAK、ALK 和 Pyk2 的酶抑制剂，具有抗肿瘤活性。Conteltinib 对 FAK 有明显的抑制作用，通过抑制 YAP 信号传导来克服肝细胞癌中缺氧介导的索拉非尼耐药性，可用于晚期 ALK 阳性非小细胞肺癌和淋巴癌。
T11126	Durvalumab MEDI 4736	PD-1/PD-L1	Apoptosis; Cell Cycle/Checkpoint; Immunology/Inflammation
	Durvalumab (MEDI 4736) 是一种人源化的抗 PD-L1 蛋白单克隆抗体，可阻断 PD-L1 与 PD-1 和 CD80 结合的能力，其 IC50 分别为 0.1 和 0.04 nM。Durvalumab 常与铂类化合物联合一起用来治疗非小细胞肺癌和晚期肝癌细胞。
T76703	Tislelizumab 替雷利珠
	Tislelizumab 是一种对PD-1受体具有高结合亲和力的单克隆抗体，可减少 Fcγ 受体与巨噬细胞的结合，从而消除抗体依赖性吞噬作用，这是一种 T 细胞清除机制，可对抗PD-1研究的潜在耐药性。Tislelizumab 可用于晚期鳞状非小细胞肺癌的研究。
T24566	O-1663 O 1663
	O-1663 is an advanced stage breast cancer inhibitor that acts by targeting multiple cannabinoid anti-tumor pathways.
T71612	SU086
	SU086 an inhibitor of HSP90, impairs glycolysis and represents a treatment strategy for advanced prostate cancer
T28237	Onapristone IVV-1001,ZK 98299,IVV 1001,ZK98299,ZK-98299,IVV1001
	Onapristone, a progesterone receptor antagonist, is used potentially for the treatment of breast cancer, advanced prostate cancer, and inducer of vaginal bleeding.
T39405	Avotaciclib trihydrochloride BEY1107 trihydrochloride
	Avotaciclib trihydrochloride, also known as BEY1107, is a highly effective and orally active inhibitor of cyclin dependent kinase 1 (CDK1). This compound is particularly valuable for researching locally advanced or metastatic pancreatic cancer.
T38050	CP-609754	Transferase	Metabolism
	CP-609754 是高效的、可逆的法尼基转移酶抑制剂，对重组人 H-Ras 和重组 K-Ras 法尼基化的 IC50分别为 0.57 ng/mL 和 46 ng/mL。CP-609754有潜在的抗癌作用。
T31837	FOLFIRI Regimen FOLFIRI
	FOLFIRI Regimen is a chemotherapy regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan used during the treatment of advanced-stage and metastatic colorectal cancer.
T21307	Heptaplatin NSC644591 NSCD644591 SKI2053R,Heptaplatin Sunpla,HTP
	Heptaplatin, a new platinum derivative with anticancer activity, is used against various cancer cell lines, including cisplatin-resistant cancer cell lines. It has been reported to have a response rate of 17% as a single agent, and tolerable toxicity in t
T3182L	L-778123 free base L-778,123,L 778123,L-778123,L778123,L 778,123
	L-778123 is an inhibitor of FPTase and GGPTase-I. The combination of L-778123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer.
T78172	PRMT5-IN-29	Histone Methyltransferase	Chromatin/Epigenetic
	PRMT5-IN-29，一种有效的口服活性PRMT5抑制剂，IC50值为1.5 μΜ，具潜力用于晚期癌症研究。
T70134	L-778123 Dihydrochloride
	L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.
T35808	C18:1 Ceramide (d18:1/18:1(9Z)) Cer(d18:1/18:1(9Z))
	C18:1 Ceramide is a naturally occurring ceramide.[1][2][3] Levels of C18:1 ceramide are elevated in overweight and insulin-resistant mice and cattle.[1][2] C18:1 Ceramide is also increased in the plasma and ovarian tissue of patients with advanced ovarian cancer. [3]
T2610	BMS-599626 AC480	EGFR; MEK; HER; Src	Angiogenesis; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors
	BMS-599626 (AC480) 是可口服的选择性 HER1和HER2抑制剂，IC50分别为 20 和 30 nM。它对 HER4 的 IC50值为 190 nM，可抑制肿瘤细胞增殖，有治疗肿瘤的潜力。
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.
T36647	Trastuzumab emtansine	Others	Others
	Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that combines the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of DM1, a microtubule-inhibitory derivative of maytansine. This compound is utilized in the investigation of advanced breast cancer[1][2].
T74415	Imlunestrant tosylate
	Imlunestrant (LY-3484356) tosylate 是口服有效且选择性的雌激素受体(estrogen receptor, ER)降解剂(SERD)，具纯拮抗性。该化合物能持续抑制ER依赖的基因转录与细胞生长，适用于研究ER阳性(ER+)晚期乳腺癌(aBC)与子宫内膜样癌(EEC)。
T76997	Socazolimab
	Socazolimab (ZKAB001) 是一种针对PD-L1的单克隆抗体，在治疗复发或转移性宫颈癌方面展现了持久的安全性和有效性。此外，Socazolimab 也被认为在小细胞肺癌、食管鳞状细胞癌 (ESCC)、晚期尿路上皮癌及骨肉瘤治疗中具有潜在应用价值。
T16354	NSC745885	Others	Others
	NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 is also an effective anti-tumor agent that displays selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 offers possibilities
T80217	BT1718	MMP	Proteases/Proteasome
	BT1718是一种针对MT1-MMP的双功能抗癌肽，通过MT1-MMP靶向肿瘤来传递细胞毒性有效载荷Mertansine。作为一种多肽-毒素偶联物，其KD值为3 nM。MT1-MMP在多种晚期实体肿瘤如三阴性乳腺癌(TNBC)和非小细胞肺癌中呈现过表达。
T68701	Abarelix acetate
	Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseli...
T71401	Oxaliplatin-d10
	Oxaliplatin-d10 is intended for use as an internal standard for the quantification of oxaliplatin by GC- or LC-MS. Oxaliplatin is a platinum-containing DNA-crosslinking agent. It induces the formation of DNA inter- and intrastrand crosslinks and DNA-protein adducts, inhibits DNA and RNA synthesis, and induces apoptosis in cancer cells. Oxaliplatin is cytotoxic to cisplatin-sensitive A2780(1A9) and KB-3-1 cells and cisplatin-resistant A2780-E(80) and KB-CP20 cells (IC50s = 0.12, 0.39, 4.7, and 2....
T72492	GnRH-R antagonist 1	GNRH Receptor	GPCR/G Protein
	GnRH-R antagonist 1 (化合物 21a) 是GnRH-R拮抗剂，具有优良口服安全性及膜透性，高亲和力结合GnRH-R（IC50=0.57 nM），并展现出有效体外拮抗活性（IC50=2.18 nM）。该化合物适用于晚期前列腺癌治疗和预防过早LH峰出现的研究。

化合物

Cat.No: T9756

Target: PARP

Cat.No: T8327

Target: Trk receptor, TAM Receptor

Cat.No: T26889

Synonym: L-4-Boronophenylalanine,4-10硼酸-L-苯丙氨酸

Target: Others

Cat.No: T30190

Target: Others

Cat.No: T2361

Synonym: LY 2874455,LY-2874455

Target: VEGFR, FGFR

Cat.No: T27259

Synonym: BOFA2,BOF A2,BOF-A2

Target: Others

Cat.No: T17216

Synonym: PSC 833

Target: P-gp

Cat.No: T15390

Synonym: D 19575,Glucosylifosfamide mustard

Target: Others

Cat.No: T11237

Synonym: Estrogen receptor antagonist 2

Target: Estrogen Receptor/ERR

Cat.No: T2145

Synonym: NSC 683864,CCI-779,西罗莫司脂化物

Target: Apoptosis, mTOR, Autophagy

Cat.No: T40199

Synonym: CPI-0209

Target: Histone Methyltransferase

Cat.No: T6084

Synonym: LY2603618,IC-83

Target: Chk, PDK, Autophagy

Cat.No: T68065

Cat.No: T39403

Synonym: BEY1107,Avotaciclib

Target: CDK

Cat.No: T2073

Synonym: GSK 2636771,GSK-2636771

Target: PI3K

Cat.No: T74698

Target: Ras

Cat.No: T6157

Synonym: CPI-613,辛酸,CPI613,CPI 613,6,8-Bis(benzylthio)octanoic acid

Target: Apoptosis, Dehydrogenase, Mitochondrial Metabolism

Cat.No: T8875

Synonym: EX-A4254,LY-3475070

Target: CD73

Cat.No: T1755

Target: GSK-3

Cat.No: T40292

Synonym: NVP-JDQ443,JDQ-443,Opnurasib

Target: Ras

Cat.No: T0078

Synonym: GSK572016,GW572016,拉帕替尼

Target: EGFR, Ferroptosis, Autophagy

Cat.No: T2381

Synonym: CDK4/6 dual inhibitor,LY2835219

Target: CDK

Lapatinib ditosylate monohydrate

Cat.No: T0078L

Synonym: Lapatinib ditosylate monohydrate,Lapatinib ditoluenesulfonate monohydrate,Lapatinib tosilate hydrate,Lapatinib tosilate,Tykerb,二甲苯磺酸拉帕替尼单水合物,Tyverb

Target: EGFR, Ferroptosis, Autophagy

Cat.No: T6883

Synonym: GTPL8918,LY3023414

Target: DNA-PK, PI3K, mTOR, Autophagy

Cat.No: T76743

Synonym: LY2875358

Target: c-Met/HGFR

Cat.No: T2283

Synonym: 2-[(1-甲基丙基)二硫代]-1H-咪唑,IV-2,PX12

Target: Thioredoxin

Cat.No: T14997

Synonym: SY-707,CT-707

Target: FAK, PYK2, ALK

Cat.No: T11126

Synonym: MEDI 4736

Target: PD-1/PD-L1

Cat.No: T76703

Synonym: 替雷利珠

Cat.No: T24566

Synonym: O 1663

Cat.No: T71612

Cat.No: T28237

Synonym: IVV-1001,ZK 98299,IVV 1001,ZK98299,ZK-98299,IVV1001

Avotaciclib trihydrochloride

Cat.No: T39405

Synonym: BEY1107 trihydrochloride

Cat.No: T38050

Target: Transferase

FOLFIRI Regimen

Cat.No: T31837

Synonym: FOLFIRI

Cat.No: T21307

Synonym: NSC644591 NSCD644591 SKI2053R,Heptaplatin Sunpla,HTP

L-778123 free base

Cat.No: T3182L

Synonym: L-778,123,L 778123,L-778123,L778123,L 778,123

Cat.No: T78172

Target: Histone Methyltransferase

L-778123 Dihydrochloride

Cat.No: T70134

C18:1 Ceramide (d18:1/18:1(9Z))

Cat.No: T35808

Synonym: Cer(d18:1/18:1(9Z))

Cat.No: T2610

Synonym: AC480

Target: EGFR, MEK, HER, Src

OB 24 hydrochloride

Cat.No: T41175

Trastuzumab emtansine

Cat.No: T36647

Target: Others

Imlunestrant tosylate

Cat.No: T74415

Cat.No: T76997

Cat.No: T16354

Target: Others

Cat.No: T80217

Target: MMP

Abarelix acetate

Cat.No: T68701

Oxaliplatin-d10

Cat.No: T71401

GnRH-R antagonist 1

Cat.No: T72492

Target: GNRH Receptor

Cat. No.	Product Name	Target	Signaling Pathways
T9715	Aplidine	SARS-CoV; DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Aplidine 是有效的eEF1A2(KD=80 nM) 靶向的抗癌药物。Aplidine 具有抗病毒活性，抑制SARS-CoV-2的 IC90为 0.88 nM。Aplidine 在多发性骨髓瘤，晚期癌症及 COVID-19 领域有研究的价值。
TN3972	Epimedokoreanin B	Apoptosis; Others; Antibacterial	Apoptosis; Microbiology/Virology; Others
	Epimedokoreanin B （EKB）是一种从韩国淫羊藿中分离出的异戊烯化类黄酮，在人非小细胞肺癌（NSCLC）A549和NCI-H292细胞中展现出抗癌活性。Epimedokoreanin B 还具有抗炎和抗菌活性，可有清除 DPPH 自由基的活性，能以剂量依赖的方式抑制 MCF-7 和 HepG2 的增殖。Epimedokoreanin B 能显著抑制 N (δ) -（羧甲基）赖氨酸（CML）和 N (Ï) -（羧甲基）精氨酸（CMA）的形成，可通过抑制高级糖化终产物（AGEs）预防糖尿病的临床并发症。
TN6059	Demethoxyfumitremorgin C
	Demethoxyfumitremorgin C and tryprostatin B are fungal inhibitors of mammalian cell cycle progression at the G(2)/M transition. Demethoxyfumitremorgin C inhibits the proliferation of PC3 human prostate cancer cells via the intrinsic (mitochondrial) and ex
TN6198	Mahanine
	Mahanine has effects on the activation of the apoptotic pathway in human leukemia U937 cells, causes the mitochondrial membranes to lose their permeability, resulting in caspase-3 activation and apoptosis. Mahanine can reverse an epigenetically silenced g

天然产物

Cat.No: T9715

Target: SARS-CoV, DNA/RNA Synthesis

Epimedokoreanin B

Cat.No: TN3972

Target: Apoptosis, Others, Antibacterial

Demethoxyfumitremorgin C

Cat.No: TN6059

Cat.No: TN6198

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