Berzosertib (VE-822) has been used in trials studying the treatment of Ovarian Neoplasms, Ovarian Serous Tumor, Adult Solid Neoplasm, Advanced Solid Tumor, and Advanced Solid Neoplasm, among others.

CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC).. CL2A-SN-38 is composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a noncleavable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. .

Dipotassium tetrachloroplatinate (Potassium tetrachloroplatinate) exhibits antitumor activity in solid tumor lines and can be used in the treatment of oncological diseases. Dipotassium tetrachloroplatinate also acts as a radiosensitizer and enhances the killing effect of thermotherapy.

AP23846 is a novel and potent Src family kinase inhibitor that reduces vascular endothelial growth factor and interleukin-8 expression and abrogates downstream angiogenic processes in human solid tumor cell lines.

Safingol hydrochloride (L-threo-dihydrosphingosine hydrochloride) is a specific inhibitor of protein kinase C. It induces autophagy in solid tumor cells and cancer cell death by inhibiting the PKC and PI3-kinase pathways.BIIB 722 Mesylate is a selective sodium-hydrogen exchange inhibitor. Safingol hydrochloride inhibits PKC and PI3k.

Pyrazoloacridine (PD 115934) is a nucleic acid binding agent that inhibits the activity of topo I and II with an IC50 of 1.25 μM in K562 cells. Pyrazoloacridine shows anti-cancer activity.

AG-270 is an allosteric and orally active inhibitor of MAT2A.

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)

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.

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

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

Naptumomab, a tumor-targeting superantigen (TTS), is a fusion protein that activates the immune system to recognize and eradicate tumor cells. It shows promise in researching refractory solid tumors, including renal cell carcinoma [1] [2].

Cinrebafusp alfa (PRS 343) is an anticalin-based bispecific drug with high affinity for both CD137/HER2, displaying dissociation constants (Kd) of 0.3 nM to recombinant human HER2 and 5 nM to human monomeric CD137 (4-1BB). It promotes T-cell costimulation via tumor-localized, HER2-mediated 4-1BB clustering and activation, thereby enhancing T-cell receptor-driven responses and facilitating tumor cell eradication. This compound shows promising potential in research concerning HER2-positive solid tumors [1] [2].

Urelumab(BMS-66513) is a humanized IgG4 monoclonal antibody, often used as a CD137 agonist.Urelumab has potential antitumor activity, potentiating tumor cell killing by T-cells and natural killer cells, and enhancing the cytotoxicity of Rituximab.Urelumab has been used in the study of solid tumor-related diseases such as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL). Urelumab can be used to study diseases associated with solid tumors such as diffuse large B-cell lymphoma (DLBCL) and follicular lymphoma (FL).

Conatumumab (AMG 655) is a monoclonal agonist antibody targeting human death receptor 5 (DR5, TRAILR2) at Kd 1 nM for long DR5 and Kd 0.8 nM for short DR5. Conatumumab induces apoptosis in a variety of tumor types through caspase activation. Conatumumab can be used to study advanced solid tumors.

Nidanilimab (CAN04) is a fully humanized IL1RAP monoclonal antibody with a Kd value of 1.10 pM. Nidanilimab has antitumor activity, cutting off the IL1α and IL1β signaling pathways and inducing the immune system to destroy tumor cells. Nidanilimab can be used to study solid cancers such as non-small cell lung cancer (NSCLC) and pancreatic ductal adenocarcinoma (PDAC).

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

ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.

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].

Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.

Pimivalimab (JTX-4014), a PD-1 inhibitor, is utilized in solid tumor research [1].

Certepetide (CEND-1), also known as iRGD, is a bifunctional cyclic peptide that enhances tumor penetration. By interacting with alphav-integrins through its RGD motif and activating NRP-1, it transforms the solid tumor microenvironment into a temporary conduit for therapeutic agents. This property facilitates Certepetide's accumulation in tumors, making it a valuable tool in researching pancreatic cancer and other solid tumors [1] [2] [3].

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)

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......

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.

Tezacitabine is a cytostatic and cytotoxic antimetabolite. Tezacitabine is a nucleoside analogue characterized by a dual mechanism of action. Tezacitabine irreversibly inhibits ribonucleotide reductase and can be incorporated into DNA during replication or repair, resulting in DNA chain termination. Tezacitabine blocks tumor cells in G1 and S phases of the cell cycle and induces apoptotic cell death. Tezacitabine has the potential to treat leukemia and solid tumors[1][2].

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.

Docetaxel trihydrate (RP-56976 Trihydrate) is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme elevations and rarely to instances of acute hepatic necrosis generally due to severe hypersensitivity reactions or sepsis.

GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.

Samotolisib (LY3023414) is an oral ATP competitive inhibitor of the class I PI3K isoforms, DNA-PK, and mTOR. Samotolisib (LY3023414) has been used in trials studying the treatment of Neoplasm, Solid Tumor, COLON CANCER, BREAST CANCER, and Advanced Cancer, among others.

Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor targeting Tubulin and HDAC, exhibiting IC50 values of 0.403 μM for HDAC1, 0.591 μM for HDAC2, 3.552 μM for HDAC3, and 0.459 μM for HDAC6. The compound induces G2 phase cell cycle arrest and promotes apoptosis. It effectively hampers the proliferation of both hematoma and solid tumor cells, diminishes tumor metastasis, and demonstrates tumor growth inhibition in a liver tumor allograft mouse model [1].

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.

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

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 differentiation to energy homeostasis and neurological processes. OTX015 has potent antiproliferative activity accompanied by c-MYC down-regulation in several tumor types, and has demonstrated synergism with the mTOR inhibitor everolimus in different models. Oral administration of OTX-015 markedly inhibited tumor growth and reduced tumor volume. OTX015 is currently in Phase 1b studies for the treatment of hematological malignancies and advanced solid tumors such as Triple Negative Breast ......

1. Crotonoside (Isoguanosine) has much more active than adenosine in reducing the blood pressure in rabbits and cats, in decreasing the tone of isolated intestinal strips of the rabbit, guinea pig and hamster and in stimulating the isolated uterus of guinea pigs and hamsters. 2. Crotonoside inhibits the growth of S-18 and Ehrlich solid tumor in mice at the optimal doses of 96 mg/kg/day x 12 and 48 mg/kg/day x 12, with 1-T/C values of 65% and 6%, respectively.

TL-895 is an ATP-competitive, and highly selective irreversible inhibitor of Bruton’s Tyrosine Kinase(BTK). TL-895 showed good potency with an IC50 of 1.5 nM and a Ki of 11.9 nM.

RBN-2397 is a potent, selective and orally active accross species NAD+ competitive PARP7 inhibitor with IC50 less than 3 nM.

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor(IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively). It has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor

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.

Dorzolamide hydrochloride (MK507 hydrochloride) is the hydrochloride salt form of dorzolamide, an inhibitor of carbonic anhydrase, a zinc-containing enzyme that catalyzes the rapid conversion of carbon dioxide and water into carbonic acid, protons and bicarbonate ions. Distributed throughout many cells and tissues, various carbonic anhydrases play important roles in mineral and metabolic homeostasis.

Venadaparib (NOV140101) (IDX-1197) is a potent, selective and orally active PARP inhibitor with IC50s of 1.4 nM and 1.0 nM for PARP1 and PARP2, respectively. Venadaparib is insensitive to PARP-5. Venadaparib prevents the repair of DNA single-strand breaks (SSBs) and can be used in solid tumor research.

Treosulfan (Treosulphan) is a bifunctional alkylating agent. It also has activity in ovarian cancer and other solid tumor types.

Latikafusp (AMG 256), a bifunctional fusion protein, combines a PD-1-targeting antibody with an IL-21 mutein, facilitating IL-21 pathway stimulation in PD-1+ cells. It aims to enhance and sustain the functionality of cytotoxic and memory T cells, thereby inducing anti-tumor immunity. This compound shows promise for research in solid tumors [1] [2].

mIDH1-IN-1 (compound 43) is a potent and selective inhibitor of mIDH1 (isocitrate dehydrogenase 1 mutant) (IC50: 961.5 nM). mIDH1-IN-1 effectively inhibits the production of 2-HG (2-hydroxyglutarate) in HT1080 cells (EC50. mIDH1-IN-1 exhibited a significant anti-proliferative effect on IDH1 mutant U-87 cells (IC50: 41.8 nM). mIDH1-IN-1 is an anti-tumor agent and can be used to study IDH1 mutant solid tumors.

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.

Hexa-N-acetylchitohexaose enhances disease resistance in crops, and can induce an increase in soybean lignification-related and antioxidant enzyme activities.Hexa-N-acetylchitohexaose is a substrate for lysozyme.Hexa-N-acetylchitohexaose possesses antitumor activity, and can inhibit the growth of solid tumors.Hexa-N-acetylchitohexaose has been shown to be an effective antitumor agent. Hexa-N-acetylchitohexaose has antitumor activity and can inhibit solid tumor growth.

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 occlusion of tumor blood vessels, cessation of tumor blood flow, and tumor necrosis.

Devimistat (6,8-Bis(benzylthio)octanoic acid) , a lipoate analog, inhibits mitochondrial enzymes pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts tumor cell mitochondrial metabolism. It has potential chemopreventive and antineoplastic activities, and has been used in trials studying the treatment of Cancer, Lymphoma, Solid Tumors, Advanced Cancer, and Pancreatic Cancer, among others.

CL2A-SN-38 consists of a CL2A linker and an anticancer compound, SN-38, which delivers active molecules within tumor cells and in the tumor microenvironment, often in conjunction with antibodies to make biologically active antibody-coupled reactive molecules (ADCs).