targeted therapy

Elimusertib (BAY-1895344) 是一种可口服的选择性ATR 抑制剂，IC50值为 7 nM。它具有抗肿瘤活性，可研究实体瘤和淋巴瘤。

GPLGIAGQ acetate 是一种 MMP2 可切割的多肽。GPLGIAGQ acetate 可用作脂质体和胶束纳米载体中的刺激敏感接头，以在光动力治疗中合成独特的 MMP2 靶向光敏剂。

DC4 can be used to synthesize antibody-drug conjugate (ADC), which is an ADC cytotoxin. DC4 can be used for targeted therapy of tumors.

The IC50s of DC4SMe on Ramos, Namalwa and HL60 s cancer cells were 1.9 nM, 2.9 nM and 1.8 nM, respectively. DC4SMe can be used for targeted therapy of tumors. DC4SMe is a phosphate prodrug of the cytotoxic DNA alkylating agent DC4 and can be used in the

(2-Pyridyldithio)-PEG4 acid is a four-unit cleavable polyethylene glycol (PEG) linker specifically designed for the synthesis of antibody-drug conjugates (ADCs)[1]. It serves as a crucial component in the conjugation of antibodies and drugs, enabling targeted drug delivery and enhanced therapeutic efficacy. This linker possesses a (2-pyridyldithio) group at one end, facilitating the attachment of the linker to the specific site on the antibody molecule. The PEG4 chain provides the necessary flexibility and biocompatibility for optimal drug release while maintaining stability throughout the circulation in the body. Ultimately, (2-Pyridyldithio)-PEG4 acid is instrumental in the development and advancement of ADCs, a promising approach in cancer therapy.

Mal-PEG4-VC-PAB-DMEA-Seco-Duocarmycin SA is an antibody-drug conjugate linker that incorporates the antitumor antibiotic Duocarmycin SA, connected through the Mal-PEG4-VC-PAB-DMEA-Seco linker, for targeted cancer therapy.

mDPR(Boc)-Val-Cit-PAB is a cleavable linker employed in antibody-drug conjugates (ADCs) [1]. This chemical compound serves as a reliable linker in the formation of ADCs, which are biopharmaceuticals that combine the specificity of monoclonal antibodies with the potency of cytotoxic drugs for targeted cancer therapy [1].

DBCO-PEG3-VC-Exatecan (compound 25) 作为一种ADC药物-连接子偶联物 (Drug-Linker Conjugate for ADC)，由具有抑制DNA拓扑异构酶I (topoisomerase I) 功能的Exatecan以及ADC连结子 (DBCO-PEG3-VC) 组成。

212Pb-DOTAMTATE是一种双功能配体，用于制备Pb212-complex。它作为针对表达SSTR的转移性神经内分泌肿瘤治疗的靶向α射线发射治疗。212Pb-DOTAMTATE单独使用或与化疗化合物联合使用可能具有积极的临床意义。

DOTAGA-FAP-2286-ALB 是 Rofapitide tetraxetan 的衍生物，是一种靶向成纤维细胞活化蛋白 (FAP) 的选择性抑制剂，IC50为67.5 nM。通过与白蛋白的相互作用，DOTAGA-FAP-2286-ALB 增强了肿瘤中的滞留时间，延长了在血液中的循环时间，并提高了放射性金属复合物的稳定性（如111In和225Ac）。该化合物有潜力应用于FAP阳性实体瘤的放射性核素治疗 (TRT) 研究。

TRBP-IN-1 (Compound 13j) 是一种口服有效的 TAR RNA 结合蛋白 2 (TRBP) 抑制剂，IC50 为 12.72 μM。TRBP-IN-1 展现出显著的抗肝细胞癌 (HCC) 活性，有效抑制 HCC 细胞（HCCLM3 细胞 IC50 为 18.96 μM；SK-Hep-1 细胞 IC50 为 16.45 μM）的增殖与转移。通过靶向 TRBP，TRBP-IN-1 调控 miRNA 生物合成并抑制致癌 miRNA 的表达，诱导 HCC 细胞的凋亡和焦亡。该化合物可用于针对 HCC 的靶向治疗研究。

BRD4-Kinases-IN-3 is a dual BRD4-Kinases inhibitor that can be used as a value-added multi-targeted chemical probe for cancer therapy.

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)

ALK-IN-12 is a highly potent and orally active inhibitor of anaplastic lymphoma kinase (ALK), demonstrating an exceptional IC50 value of 0.18 nM. Additionally, ALK-IN-12 displays inhibitory activity against insulin-like growth factor 1 receptor (IGF1R) and insulin receptor (InsR), with IC50 values of 20.3 nM and 90.6 nM, respectively. Notably, its antitumor effects have been observed, making it a promising compound for targeted cancer therapy.

Tunlametinib是高选择性口服MEK1/MEK2激酶抑制剂（对MEK1的IC50为1.9 nM），通过阻断RAS-RAF-MEK-ERK致癌信号通路诱导肿瘤细胞周期阻滞与凋亡。对BRAF V600E或KRAS G12C等突变型肿瘤细胞具有强抑制活性，与BRAF/KRASG12C/SHP2抑制剂及多西他赛（Docetaxel）联用呈现协同效应，目前已应用于黑色素瘤、结直肠癌及非小细胞肺癌等RAS/RAF驱动型肿瘤的靶向治疗。

DOTA Zoledronate represents a novel, advanced compound utilized specifically in bone-targeted radionuclide therapy to diagnose bone metastases.

DDR1-IN-5 is a potent and selective inhibitor of the Discoidin Domain Receptor family, member 1 (DDR1). It effectively inhibits the phosphorylation of DDR1b (Y513) with an IC 50 value of 4.1 nM. Furthermore, DDR1-IN-5 demonstrates remarkable anti-cancer activity. Its inhibitory potency against DDR1 (IC 50 = 7.36 nM) makes it a promising compound for targeted therapy in cancer treatment.

Ganglioside GD3 disodium salt is a melanoma-associated antigen often targeted in immune therapy for melanomas.

NOTA是一种多功能螯合剂，能够与金属离子形成稳定络合物，常用于放射性药物、分子成像和靶向核治疗。

Antitumor agent-70 (compound 8b) is a highly potent multi-targeted kinase inhibitor, particularly targeting c-Kit. It demonstrates remarkable anti-tumor activity and the ability to induce cell apoptosis. This compound also exhibits strong inhibition of multiple myeloma, with an IC 50 value of 0.12 μM. Therefore, Antitumor agent-70 holds great potential as an effective therapy for combating cancer, especially in cases involving c-Kit. [1]

Ar-V7-IN-1（compound 47）是一种有效的 Ar-V7 抑制剂。AR-V7 是雄激素受体（AR）的一种基因mRNA剪接变异体，与去势抵抗性前列腺癌（mCRPC）患者对AR靶向治疗的耐药性相关。

OCID-4681 is a novel class-selective HDAC inhibitor for targeted therapy of cancer.

OSu-Glu-VC-PAB-MMAD是由微管抑制剂MMAD与可降解的ADC linker OSu-Glu-VC-PAB通过一种高度特异性的连接方式构成，作为抗体-活性分子偶联物（antibody-drug conjugates, ADCs）中的关键组成部分。

MC-VC-PABC-SP 141 是抗体-活性分子偶联物的一部分，由有效的 MDM2抑制剂 SP 141 和可降解的 ADC linkerMC-VC-PABC 连接而成。