solid tumor

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。

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。

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)。

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。

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。

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) 。

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。

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。

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。

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。

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。

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。

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。

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。

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。

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。

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。

Pimivalimab (JTX-4014) 是一种PD-1抑制剂。Pimivalimab 可用于实体瘤的研究。

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。

2-deoxy-D-Glucose-13C6is intended for use as an internal standard for the quantification of 2-deoxy-D-glucose by GC- or LC-MS. 2-deoxy-D-Glucose is a glucose antimetabolite and an inhibitor of glycolysis.1,2It inhibits hexokinase, the enzyme that converts glucose to glucose-6-phosphate, as well as phosphoglucose isomerase, the enzyme that converts glucose-6-phosphate to fructose-6-phosphate.32-deoxy-D-Glucose (16 mM) induces apoptosis in SK-BR-3 cells, as well as inhibits the growth of 143B osteosarcoma cells cultured under hypoxic conditions when used at a concentration of 2 mg ml.4,5In vivo, 2-deoxy-D-glucose (500 mg kg) reduces tumor growth in 143B osteosarcoma and MV522 non-small cell lung cancer mouse xenograft models when used alone or in combination with doxorubicin or paclitaxel .6 1.Kang, H.T., and Hwang, E.S.2-Deoxyglucose: An anticancer and antiviral therapeutic, but not any more a low glucose mimeticLife Sci.78(12)1392-1399(2006) 2.Aft, R.L., Zhang, F.W., and Gius, D.Evaluation of 2-deoxy-D-glucose as a chemotherapeutic agent: Mechanism of cell deathBr. J. Cancer87(7)805-812(2002) 3.Ralser, M., Wamelink, M.M., Struys, E.A., et al.A catabolic block does not sufficiently explain how 2-deoxy-D-glucose inhibits cell growthProc. Natl. Acad. Sci. USA105(46)17807-17811(2008) 4.Liu, H., Savaraj, N., Priebe, W., et al.Hypoxia increases tumor cell sensitivity to glycolytic inhibitors: A strategy for solid tumor therapy (Model C)Biochem. Pharmacol.64(12)1745-1751(2002) 5.Zhang, X.D., Deslandes, E., Villedieu, M., et al.Effect of 2-deoxy-D-glucose on various malignant cell lines in vitroAnticancer Res.26(5A)3561-3566(2006) 6.Maschek, G., Savaraj, N., Priebe, W., et al.2-deoxy-D-glucose increases the efficacy of adriamycin and paclitaxel in human osteosarcoma and non-small cell lung cancers in vivoCancer Res.64(1)31-34(2004)

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 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D......

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-containing nanoparticles.4,5 1.Sloat, B.R., Sandoval, M.A., Li, D., et al.In vitro and in vivo anti-tumor activities of a gemcitabine derivative carried by nanoparticlesInt. J. Pharm.409(1-2)278-288(2011) 2.Abd-Rabou, A.A., Bharali, D.J., and Mousa, S.A.Taribavirin and 5-fluorouracil-loaded pegylated-lipid nanoparticle synthesis, p38 docking, and antiproliferative effects on MCF-7 breast cancerPharm. Res.35(4)76(2018) 3.Affram, K., Udofot, O., Singh, M., et al.Smart thermosensitive liposomes for effective solid tumor therapy and in vivo imagingPLoS One12(9):e0815116(2017) 4.Wang, L.-S., Wu, L.-C., Lu, S.-Y., et al.Biofunctionalized phospholipid-capped mesoporous silica nanoshuttles for targeted drug delivery: Improved water suspensibility and decreased nonspecific protein bindingACS Nano4(8)4371-4379(2010) 5.Wen, X., Wang, K., Zhao, Z., et al.Brain-targeted delivery of trans-activating transcriptor-conjugated magnetic PLGA/lipid nanoparticlesPLoS One9(9):e106652(2014)

Tezacitabine 是一种抑制细胞生长和细胞毒性的抗代谢物。 Tezacitabine 是一种核苷类似物，具有双重作用机制。 Tezacitabine 不可逆地抑制核糖核苷酸还原酶，并可在复制或修复过程中掺入 DNA，导致 DNA 链终止。 Tezacitabine 在细胞周期的 G1 期和 S 期阻断肿瘤细胞并诱导凋亡细胞死亡。 Tezacitabine 具有治疗白血病和实体瘤的潜力[1][2]。

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 Pfeiffer.

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 majority of human carcinomas of all types, arises from a blockage in the normal O-glycosylation pathway in which glycans are extended from the common precursor GalNAcα1-O-Ser/Thr (Tn +antigen)[1].

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.

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.

Tessaric acid has antifeedant and allelochemical effects. Tessaric acid derivatives induce G/M cell cycle arrest in human solid tumor cell lines.

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。

Rezatapopt (PC14586) 是一种小分子 p53 重激活剂，具有抗肿瘤活性，选择性地结合 TP53 Y220C 突变蛋白中存在的缝隙，并恢复 p53 野生型（正常）构象和转录活性，可用于研究局部晚期或转移性实体瘤。

VVD-130037 是靶向 KEAP1 的，具有口服生物活性的小分子激活剂。VVD-130037 可促使 NRF2 泛素化降解，从而抑制晚期实体瘤的肿瘤生长。

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。

Venadaparib hydrochloride (IDX-1197) is a potent and selective PARP inhibitor that exhibits significant anticancer properties. It is particularly effective in solid tumor research.

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 substrate. It inhibited microtubule assembly followed by M-phase arrest, Bcl-2 inactivation, and then apoptosis through caspase pathways.

Pierreione B is an inhibitor of mTOR signaling with strong anticancer activity. Pierreione A and Pierreione B demonstrate solid tumor selectivity with minimal cytotoxicity.

Bithionol sulfoxide is a clinically approved antiparasitic drug with the inhibitory against solid tumor growth in several preclinical cancer models.

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。

Anticancer agent 48 (compound 48) 是一种广谱抗癌剂，其表现出抗增殖活性。Anticancer agent 48 对微管蛋白聚合具有抑制作用。Anticancer agent 48 在体内显示抗肿瘤活性。Anticancer agent 48 具有潜力进行实体瘤和血液肿瘤的研究。主语

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。

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].

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 this compound also induced depolymerization of preassembled microtubules. Cell cycle analysis of tumor cell lines treated with LU103793 indicated a block in the G2-M phase.

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。

ARI-3144 是一种成纤维细胞激活蛋白 (FAP) 的优良底物，同时也是一种FAP激活的蛋白酶体抑制剂，适用于实体瘤研究。

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。

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.

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。

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。

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。