53
4
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9050 |
AG-270
|
Others; Methionine Adenosyltransferase (MAT) | Chromatin/Epigenetic; Others |
AG-270 是一种可逆的、非竞争性的、具有口服活性的MAT2A 变构抑制剂(IC50:14 nM)。 | |||
T12695 |
RBN-2397
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
RBN-2397 是一种有效的、选择性的、具有口服活性的跨物种 NAD+ 竞争性 PARP7 抑制剂,IC50 小于 3 nM。它选择性结合 PARP7 ,Kd 为0.001 μM,可恢复干扰素 I 型信号转导,有用于晚期或转移性实体肿瘤的研究潜力。 | |||
T9705 |
TL-895
|
BTK | Angiogenesis; Tyrosine Kinase/Adaptors |
TL-895 是口服有效的,ATP 竞争性的,以及高度选择性和不可逆的BTK 抑制剂,IC50和Ki 分别为 1.5 nM 和 11.9 nM。TL-895在 JAKi 复发/难治性骨髓纤维化、急性髓系白血病、COVID-19 和癌症方面有研究的价值。 | |||
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。 | |||
T6079 |
NVP-ADW742
ADW742,ADW,GSK 552602A |
Apoptosis; IGF-1R | Apoptosis; Tyrosine Kinase/Adaptors |
NVP-ADW742 (ADW) 是一种具有口服活性,选择性的IGF-1R 酪氨酸激酶抑制剂,IC50为 0.17 μM。它抑制胰岛素受体,IC50为 2.8 μM,在肿瘤细胞中诱导多效性抗增殖/促凋亡。 | |||
T28475 |
Pyrazoloacridine
PD-115934,NSC 366140,NSC-366140,PD 115,934,PD 115934 |
Apoptosis; Topoisomerase | Apoptosis; DNA Damage/DNA Repair |
Pyrazoloacridine (PD 115934) 是一种核酸结合剂,在 K562 细胞中抑制 topo I 和 II 的活性,IC50 为 1.25 μM。 Pyrazoloacridine 具有抗癌活性。 | |||
T2134 |
Dorzolamide hydrochloride
MK507 hydrochloride,L671152 hydrochloride,MK-507 (L-671152) HCl,盐酸多佐胺,Dorzolamide HCl |
Carbonic Anhydrase | Metabolism |
Dorzolamide hydrochloride (MK507 hydrochloride) 是一种碳酸酐酶carbonic anhydrase II 抑制剂,能够抑制红细胞CA-II(IC50:0.18 nM) 和CA-I(IC50:600 nM) 。 | |||
T2669 |
Berzosertib
VX-970,VE-822 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Berzosertib (VE-822) 已用于研究卵巢肿瘤、卵巢浆液性肿瘤、成人实体瘤、晚期实体瘤和晚期实体瘤等治疗的试验。 | |||
T2357 |
GSK1059615
GSK 1059615,GSK-1059615 |
Apoptosis; PI3K; mTOR | Apoptosis; PI3K/Akt/mTOR signaling |
GSK1059615 是一种 PI3Kα/β/δ/γ可逆的抑制剂,同时也抑制 mTOR,IC50值分别为 0.4 nM/0.6 nM/2 nM/5 nM 和 12 nM,已用于研究淋巴瘤、实体瘤、子宫内膜癌、实体瘤癌和转移性乳腺癌治疗的试验。 | |||
T17159 |
Treosulfan
NSC 39069,曲奥舒凡,Treosulphan |
DNA Alkylator/Crosslinker; DNA Alkylation | DNA Damage/DNA Repair |
Treosulfan (Treosulphan) 是一种双功能的烷化剂,对卵巢癌及其他的实体瘤都有抑制效果。 | |||
T3709 |
XMD8-87
ACK1-B19 |
Tyrosinase; PPAR | DNA Damage/DNA Repair; Metabolism; Proteases/Proteasome |
XMD8-87 (ACK1-B19)是TNK2抑制剂,对于D163E 和R806Q 突变体的IC50值分别为38和113 nM。 | |||
T1962 |
ASP3026
ASP 3026 |
Apoptosis; ALK | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
ASP3026 是一种选择性的,具有口服活性的间变性淋巴瘤激酶抑制剂,可诱导肿瘤细胞凋亡,可研究非小细胞肺癌。 | |||
T77367 |
Urelumab
BMS-663513,BMS-66513 |
Others | Others |
Urelumab(BMS-66513) 是一种人源化的 IgG4 单克隆抗体,常被当作 CD137 激动剂使用。Urelumab 具有潜在的抗肿瘤活性,可增强 T 细胞和自然杀伤细胞对肿瘤细胞的杀伤作用,并增强 Rituximab 的细胞毒性。Urelumab 可用于研究弥漫性大B细胞淋巴瘤 (DLBCL)合滤泡性淋巴瘤 (FL) 等实体瘤相关疾病。 | |||
T68455 |
AP23846
AP-23846 |
Src | Angiogenesis; Tyrosine Kinase/Adaptors |
AP23846 是一种新型高效的 Src 家族激酶抑制剂,可降低人实体瘤细胞系中血管内皮生长因子和白细胞介素-8 的表达,并消除下游血管生成过程。 | |||
T77688 |
Dipotassium tetrachloroplatinate
Potassium tetrachloroplatinate |
Others | Others |
Dipotassium tetrachloroplatinate (Potassium tetrachloroplatinate) 在实体肿瘤系中表现出抗肿瘤活性,可用于有治疗肿瘤疾病。Dipotassium tetrachloroplatinate 还可充当放射增敏剂,可增强热疗杀伤作用。 | |||
T1890 |
Pracinostat
SB939 |
Apoptosis; HDAC | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair |
Pracinostat (SB939) 是一种组蛋白去乙酰化酶抑制剂,对 HDACs 的IC50值为 40-140 nM,可用于研究癌症。 | |||
T83978 |
Safingol hydrochloride
SPC 100270 hydrochloride,L-threo-dihydrosphingosine hydrochloride |
PI3K; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) 是蛋白激酶 C 特异性抑制剂,通过抑制 PKC 和 PI3-激酶途径诱导实体瘤细胞自噬,诱导癌细胞死亡。Safingol hydrochloride 抑制 PKC 和 PI3k。 | |||
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。 | |||
T9430 |
Venadaparib
NOV140101,IDX-1197 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Venadaparib (NOV140101) 是一种选择性和具有口服活性的 PARP 抑制剂,对 PARP1和 PARP2的 IC50分别为 1.4 和 1.0 nM。它可防止 DNA 单链断裂 (SSB) 的修复,可研究实体瘤。 | |||
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。 | |||
T5058 |
Pamiparib
BGB-290 |
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
Pamiparib (BGB-290) 是一种具有口服活性、强效、高选择性的 PARP 抑制剂,对PARP1和PARP2的IC50值分别为 0.9 nM 和 0.5 nM。它具有强大的 PARP 捕获能力,具有穿透大脑的能力,可用于研究癌症。 | |||
T76787 |
Conatumumab
TRAIL-R2 mAb,AMG 655 |
TNF | Apoptosis |
Conatumumab (AMG 655) 是一种靶向人死亡受体 5 (DR5,TRAILR2) 的单克隆激动剂抗体 ,对长型 DR5 的 Kd 为 1 nM, 对短型 DR5 的 Kd 0.8 nM。Conatumumab 通过半胱天冬酶激活在多种肿瘤类型中诱导细胞凋亡。Conatumumab 可用于研究晚期实体肿瘤。 | |||
T76873 |
Nidanilimab
CAN04 |
IL Receptor | Immunology/Inflammation |
Nidanilimab (CAN04) 是一种完全人源化的 IL1RAP 单克隆抗体,其 Kd 值为 1.10 pM。Nidanilimab 具有抗肿瘤活性,切断 IL1α 和 IL1β 信号通路,并诱导免疫系统破坏肿瘤细胞。Nidanilimab 可用于研究非小细胞肺癌 (NSCLC) 和胰腺导管腺癌 (PDAC) 等实体癌。 | |||
T9972 |
Divarasib
GDC-6036 |
Ras | GPCR/G Protein; MAPK |
Divarasib (GDC-6036) (GDC-6036)是一种正在研究的、口服的、高效力和选择性的 KRAS G12C 抑制剂,IC50 为 <0.01 μM。Divarasib 不可逆地将 KRAS G12C 癌蛋白锁定在非活性状态,抑制肿瘤细胞生长。它正在被研究用于实体肿瘤,包括非小细胞肺癌和结肠直肠癌及其他类型的癌症。 | |||
T17731L |
CL2A-SN-38 DCA 1279680-68-0(free base)
|
Others | Others |
CL2A-SN-38 DCA 1279680-68-0(free base) 是一种药物-接头偶联物,由有效的 DNA 拓扑异构酶 I 抑制剂 SN-38 和接头 CL2A 组成,用于制造抗体药物偶联物 (ADC)。CL2A-SN-38 由有效的 DNA 拓扑异构酶组成I 抑制剂 SN-38 和接头 CL2A 以制造抗体药物偶联物 (ADC)。 CL2A-SN-38 对一系列人类实体瘤类型提供显着和特异性的抗肿瘤作用。 CL2A 是一种不可切割的复杂 PEG8 和含有三唑的 PABC-肽-mc 接头。 CL2A 可通过 pH 敏感性裂解,产生旁观者效应,并通过二硫键在半胱氨酸残基处结合抗体。 | |||
T10551 | Bithionol sulfoxide | Others | Others |
Bithionol sulfoxide is a clinically approved antiparasitic drug with the inhibitory against solid tumor growth in several preclinical cancer models. | |||
T28310 |
PD 114595
PD-114595,PD114595 |
||
PD 114595 is a Benzothiopyrano-indazole cpd. PD 114595 belongs to a class of DNA complexers, PD 114595 has curative properties against murine solid tumor models. | |||
T39147 |
Venadaparib hydrochloride
IDX-1197 hydrochloride |
||
Venadaparib hydrochloride (IDX-1197) is a potent and selective PARP inhibitor that exhibits significant anticancer properties. It is particularly effective in solid tumor research. | |||
T77164 | Pimivalimab | ||
Pimivalimab (JTX-4014) 是一种PD-1抑制剂。Pimivalimab 可用于实体瘤的研究。 | |||
TP2468 |
PNU-145156E (FCE26644)
FCE 26644,FCE26644,PNU-145156E,PNU145156E,FCE-26644,PNU 145156E |
||
PNU-145156E (FCE26644) a novel angiogenesis inhibitor, has been shown to block circulating angiogenesis promoting growth factor in animal studies and has shown anti-tumor effects in solid tumors in mice. | |||
T68708 |
Denibulin HCl
|
||
Denibulin (MN-029) is a novel vascular-disrupting agent that reversibly inhibits microtubule assembly, resulting in disruption of the cytoskeleton of tumor vascular endothelial cells. The results of preclinical study demonstrated that MN-029 could cause rapid vascular shutdown in solid tumors, dose-dependent secondary tumor cell killing, and effective enhancement of the antitumor effects of radiation and cisplatin chemotherapy. | |||
T69813 |
AZD-6126
|
||
AZD6126, also known as ANG-453, a water-soluble phosphate prodrug of N-acetylcolchinol with potential antiangiogenesis and antineoplastic activities. AZD-6126 is an angiogenesis inhibitor and tubulin inhibitor potentially for the treatment of solid tumours. AZD6126 is converted in vivo into N-acetylcolchinol. N-acetylcolchinol binds to and destabilizes the tubulin cytoskeleton of endothelial cells in tumor blood vessels, which may result in tumor endothelial cel apoptosis, the selective occlusio... | |||
T81704 |
Naptumomab
|
||
Naptumomab是一种针对肿瘤细胞的超级抗原(TTS)融合蛋白。它能激活免疫系统,使之识别并消灭肿瘤细胞。该化合物主要应用于肾细胞癌等难治性实体肿瘤的研究领域。 | |||
T76255 |
Certepetide
|
||
Certepetide (CEND-1),即双功能环肽(a.k.a. iRGD),是一种具有穿透肿瘤功能的多肽。通过与α-V整联蛋白(alphav-integrins)的RGD motif相互作用,以及激活神经纤毛蛋白1(NRP-1),Certepetide能够将实体瘤微环境转化成临时的活性分子通道,从而在肿瘤中累积。该化合物在胰腺癌和其他实体瘤的研究中具有应用潜力。 | |||
T61370 |
DNA-PK-IN-6
|
||
DNA-PK-IN-6, a robust DNA-PK inhibitor, effectively hampers the activity of DNA-PKcs, thereby significantly impairing the DNA repair mechanism in tumors and instigating apoptosis in cells. Additionally, DNA-PK-IN-6 amplifies the responsiveness of tumor tissues to radiotherapy, overcomes the challenge of drug resistance, and augments its inhibitory impact on a diverse range of solid and hematological tumors[1]. | |||
T40486 |
Hexa-N-acetylchitohexaose
N-Acetylchitohexaose |
Others | Others |
Hexa-N-acetylchitohexaose 可加强农作物的抗病性,可促使大豆木质化相关酶和抗氧化酶活性增加。Hexa-N-acetylchitohexaose 是溶菌酶的底物。Hexa-N-acetylchitohexaose 具有抗肿瘤活性,可抑制实体肿瘤生长。 | |||
T69766 | Gusacitinib HCl | ||
Gusacitinib, also known as ASN-002 and EN-3351, is a potent dual inhibitor of SYK/JAK kinases. ASN002 showed strong antitumor activity in both hematological and solid tumor xenograft models. ASN002 strongly suppressed the SYK and JAK family kinase signaling pathways as measured in pLAT and pSTAT assays, respectively. When profiled in a panel of 178 cell lines, ASN002 showed strong anti-proliferative activity in many lymphoid/leukemia cell lines, including SU-DHL-6, SU-DHL-4, OCI-LY10, H929 and... | |||
T79452 |
Tubulin/HDAC-IN-2
|
||
Tubulin/HDAC-IN-2 (Compound II-19k) 为Tubulin和HDAC的双重抑制剂,IC50分别对HDAC1、HDAC2、HDAC3和HDAC6为0.403 μM、0.591μM、3.552μM和0.459μM。该化合物能够导致细胞周期在G2期的阻滞及诱导细胞凋亡。Tubulin/HDAC-IN-2 有效抑制血肿和实体瘤细胞增殖,降低肿瘤转移,并在肝肿瘤同种异体移植的小鼠模型中抑制肿瘤生长。 | |||
T74542 | YM458 | Histone Methyltransferase | Chromatin/Epigenetic |
YM458为EZH2和BRD4的有效双重抑制剂,IC50值分别为490 nM和34 nM。该化合物能够抑制实体癌细胞的增殖与集落形成,并诱导细胞周期阻滞与细胞凋亡(apoptosis),适用于抗癌研究领域。 | |||
T70235 |
Cemadotin hydrochloride
|
||
Cemadotin hydrochloride is the salt from of Cemadotin (free base), also known as, LU103793, a mitosis inhibitor potentially for the treatment of solid tumours. Cemadotin is also a synthetic derivative of Dolastatin 15, an antiproliferative compound which was isolated from the mollusk Dolabella auricularia. Like Dolastatin 15, LU103793 is highly cytotoxic in vitro (IC50 = 0.1 nM). LU103793 inhibits microtubule polymerization in a concentration-dependent manner (IC50 = 7 microM). Treatment with ... | |||
T69963 |
Birabresib dihydrate
|
||
Birabresib dihydrate was initially developed by Mitsubishi Tanabe Pharma Corporation, but then was licensed by OncoEthix, privately held biotechnology company. OTX015 is a selective bromodomains: BRD2, BRD3, and BRD4 inhibitor and inhibits their binding to AcH4. Bromodomains have an important role in the targeting of chromatin-modifying enzymes to specific sites, including methyltransferases, HATs and transcription factors and regulate diverse biological processes from cell proliferation and dif... | |||
T68389 | LY2457546 | ||
LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 synge... | |||
T78528 |
ERX-41
|
Others | Others |
ERX-41是一种口服活性的立体特异性小分子,靶向溶酶体酸性脂肪酶A (LIPA)。该化合物通过诱导内质网(ER)应激从而导致细胞死亡,这一作用表明ERX-41功能独立于LIPA,但依赖于其在内质网的定位。ERX-41主要用于实体瘤靶向研究。 | |||
T80590 |
Cinrebafusp alfa
PRS 343 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Cinrebafusp alfa (PRS 343) 是高亲和力 CD137/HER2 双特异性抗体融合蛋白,能结合重组人 HER2 (Kd=0.3 nM) 及人单体 CD137 (4-1BB; Kd=5 nM)。通过 HER2 导向的 4-1BB 聚集激活,Cinrebafusp alfa 促进 T 细胞的共刺激作用,增强 T细胞受体介导的活性,从而有效打击 HER2+ 实体瘤。 | |||
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... | |||
T77052 | Latikafusp | ||
Latikafusp (AMG 256)是一种靶向PD-1+细胞的双功能融合蛋白,整合了针对PD-1的抗体及IL-21突变蛋白,用于提供IL-21通路的刺激。通过启动和延长细胞毒性及记忆T细胞的活性,该蛋白质能够诱导抗肿瘤免疫反应,显示出对实体瘤研究的应用潜力。 | |||
T64475 |
FMOC-L-THR
|
||
FMOC-L-THR (AZP-531) is an analogue of unacylated ghrelin designed to improve glycaemic control and reduce weight. The O-glycosidic linkage and the O-acetyl protection in this building block is stable to both piperidine and TFA, making it completely compatible with standard protocols in Fmoc solid phase peptide synthesis. The Tn antigen is a tumor-associated carbohydrate antigen that is not normally expressed in peripheral tissues or blood cells. Expression of this antigen, which is found in a m... | |||
T36424 |
DSPE-PEG(2000)-amine (sodium salt)
|
||
DSPE-PEG(2000)-amine is a PEGylated derivative of 1,2-distearoyl-sn-glycero-3-PE . It has been used in the synthesis of solid lipid and thermosensitive liposomal nanoparticles for the delivery of anticancer agents.1,2,3DSPE-PEG(2000)-amine has also been used in the synthesis of fluorescein isothiocyanate-loaded mesoporous silica nanoparticles for imaging applications.4It can be conjugated to a variety of functional molecules for improved cellular targeting and uptake of DSPE-PEG(2000)-amine-cont... | |||
T62698 | mIDH1-IN-1 | ||
mIDH1-IN-1 (compound 43) 是一种有效的、选择性的 mIDH1 (异柠檬酸脱氢酶 1 突变体) 抑制剂 (IC50: 961.5 nM)。mIDH1-IN-1 可以有效抑制 HT1080 细胞内 2-HG (2-hydroxyglutarate) 的产生 (EC50: 208.6±8.0 nM)。mIDH1-IN-1 对 IDH1 突变体 U-87 细胞表现出明显的抗增殖效果(IC50: 41.8 nM)。mIDH1-IN-1 是一种抗肿瘤剂,能够用于研究 IDH1 突变实体瘤。 | |||
T17731 |
CL2A-SN-38
|
Others | Others |
CL2A-SN-38 是一种药物-接头偶联物,由一种有效的 DNA 拓扑异构酶 I 抑制剂 SN-38 和接头 CL2A 组成,用于制造抗体药物偶联物。它对一系列人类实体瘤类型提供显着和特异性的抗肿瘤作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6S0033 |
Crotonoside
巴豆苷;异鸟苷,巴豆苷,Isoguanosine,2-HYDROXYADENOSINE |
Others; FLT; HDAC | Angiogenesis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Others; Tyrosine Kinase/Adaptors |
Crotonoside (Isoguanosine) 是从中草药巴豆中分离出来的一种天然产物。 它抑制 FLT3 和 HDAC3/6,有治疗急性髓性白血病 (AML)的研究潜力。 | |||
T0186 |
Docetaxel trihydrate
RP-56976 (Trihydrate),RP56976 (NSC 628503) Trihydrate,多西他赛三水合物 |
Apoptosis; BCL; Microtubule Associated | Apoptosis; Cytoskeletal Signaling |
Docetaxel trihydrate (RP-56976 Trihydrate) 是一种抗肿瘤试剂,抑制微管解聚的IC50值为 0.2 μM。它是紫杉醇的半合成类似物,能减弱 bcl-2 和 bcl-xL 基因表达的影响。它阻滞G2/M 细胞周期,导致细胞凋亡。 | |||
TN6511 |
Tessaric acid
|
||
Tessaric acid has antifeedant and allelochemical effects. Tessaric acid derivatives induce G/M cell cycle arrest in human solid tumor cell lines. | |||
TN4788 |
Pierreione B
|
mTOR | PI3K/Akt/mTOR signaling |
Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity. |