cancers

Trastuzumab is a humanized monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab has been clinically used to treat HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer.

Trastuzumab deruxtecan (T-DXd) is an antibody-activated molecule coupling (ADC) with anticancer and antitumour activity.Trastuzumab deruxtecan has been shown to have an ameliorative effect in HER2-positive breast and gastric cancers.

Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.

Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.

N-Nitroso-N-methylurea is a nitrosourea compound with alkylating, carcinogenic and mutagenic properties. It targets a variety of animal organs, causes various cancers and degenerative diseases, and can be used in diazomethane synthesis.

mTOR inhibitor 9b is an enzyme inhibitor of protein kinase mTOR he phosphatidylinositol 3-kinase PIK3CA with IC50s of 0.76 nm and 1.262 µM, respectively.mTOR inhibitor 9b possesses anticancer activity and can be used to study leukemia, skin, breast, lung and colon cancers.

IFB-088 acetate, a benzyl guanidine derivative, is used to treat diseases and cancers associated with the PPP1R15A pathway and associated with protein misfolding stress, Examples include tau disease, synaptic riboprotein disease, polyglutamine and polyalanine diseases, leukodystrophy, cystic fibrosis, multiple sclerosis, lysosome storage disorders, amyloidosis diseases, inflammation, metabolic disorders, cardiovascular diseases, osteoporosis, neurological trauma, and more.

BTK-IN-16 is a potential inhibitor of wild-type BTK and C481S mutants.BTK-IN-16 can be used to study various autoimmune diseases and cancers caused by BTK.

FGFR2-IN-1 is an FGFR inhibitor that inhibits FGFR1, FGFR2, and FGFR3 with IC50s of 460, 140, and 2200 nM, respectively.FGFR2-IN-1 can be used for the study of cancers associated with FGFR2.CAS 번호13460-73-81-1

6-methyl-2-[2-[(E)-(6-oxo-1-cyclohexa-2,4-dienylidene)methyl]hydraziny l]-1H-pyrimidin-4-one (NSC 73150) is a pyrimidine derivative with antitumor activity. Preclinical studies have shown that it inhibits the growth of a variety of tumor cell lines, including breast, lung, and liver cancers. It has also been found to induce apoptosis, inhibit angiogenesis and suppress tumor metastasis.

ARTD10/PARP10-IN-1 is a potent PARP inhibitor of the mono-ADP ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly ADP-ribose polymerase-1 (ARTD1/PARP1), with potential anticancer and antitumour activity for the study of prostate and breast cancers.

Triptorelin acetate(57773-63-4 free base) (CL 118,532) is used as a GnRH agonist. It decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle-stimulating hormone (FSH) by causing constant stimulation of the pituitary. Triptorelin acetate(57773-63-4 free base) may be used in the treatment of hormone-responsive cancers such as breast cancer or prostate cancer, precocious puberty, estrogen-dependent conditions, and assisted reproduction.

GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.

UUN44923 is a FTO inhibitor. It may be useful for treating diseases assocd. with FTO targets, obesity, metabolic syndrome (MS) , type 2 diabetes (T2D) , Alzheimer's diseases, breast cancers, small- cell lung cancers, a human bone marrow striated muscle cancer, a pancreatic cancer, malignant glioblastoma and the like.

Ras Inhibitory Peptide acetate is a peptide involved in the Ras-dependent signaling pathway that plays an important role in human cancers initiated by oncogenic receptors.

MS8511 HCl is a selective and potent covalent inhibitor of G9a/GLP that acts by targeting cysteine residues in the substrate binding site. MS8511 has anticancer activity and antiproliferative activity and reduces intracellular H3K9me2 levels.MS8511 can be used to study a wide range of cancers including brain, breast, and ovarian cancers .

Pegamotecan (PEG-camptothecin) is a topoisomerase I (TOP1) inhibitor with anticancer activity, and it is used in the treatment of esophageal, non-small cell lung and pancreatic cancers.

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Zavondemstat (QC8222 free base) is a histone lysine demethylase 4 (KDM4) inhibitor with anticancer and antitumor activity for the study of triple-negative and breast cancers.

MS8511, a selective covalent irreversible inhibitor of G9a/GLP, targets a cysteine residue at the substrate binding site, displaying IC50 values of 100 nM (G9a) and 140 nM (GLP), alongside Kd values of 44 nM (G9a) and 46 nM (GLP). This compound effectively reduces cellular H3K9me2 levels and boosts antiproliferation activity, making it applicable in cancer research involving brain, breast, ovarian, lung, bladder, melanoma, and colorectal cancers, as well as studies on Alzheimer’s disease (AD), sickle cell disease, and Prader−Willi syndrome (PWS) [1].

IRAK4-IN-10 is a potent IRAK4 inhibitor (IC50: 1.5 nM) with potential anticancer and anti-inflammatory activities.IRAK4-IN-10 blocks MyD88 signaling and can be used for the study of autoimmune diseases and cancers.

Cancer-Targeting Compound 1 can be used in the study of hormone-related cancers, including the treatment or prevention of fibroids, uterine leiomyomas, polycystic ovarian syndrome, or hormone-dependent Cancer, among others.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively[1]. The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg/kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg/kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1]. [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

Proanthocyanidins is a natural product, used as antioxidant and anti-cancers agent.

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

DGKζ-IN-4 is a DGK-zeta inhibitor employed as an active ingredient in pharmaceutical formulations designed to treat cancers linked to immune cell activation or those resistant to anti-PD-1/anti-PD-L1 antibody treatments [1].

SMP-33693 is an Antibody-Drug Conjugate (ADC) known for its low payload shedding rate and demonstrated in vivo tumor inhibition in ovarian, gastric, and breast cancers [1].

MC-VC-PABC-C6-alpha-Amanitin is an antibody-drug conjugate that combines the anticancer toxin alpha-Amanitin with the monoclonal antibody MC-VC-PABC-C6. Alpha-Amanitin acts as a potent inhibitor of RNA polymerase IIα, enabling the conjugate to selectively target and recognize HER2-positive tumor cells. This specificity makes MC-VC-PABC-C6-alpha-Amanitin a valuable research tool in the study of breast and gastric cancers [1].

Antiproliferative agent-26 (compound 4g) exhibits a broad spectrum of activity against leukemia, CNS cancers, melanoma, renal, and breast cancers at a concentration of 10 μM. It hinders colony formation and induces cell cycle arrest in the G1 phase at 5 μM, while arresting the cell cycle at the S phase at 25 μM [1].

Oncopterin is found in urine from patients with solid and blood cancers.

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)

Chamaejasmenin B is a compound isolated from Stellera chamaejasme L. Chamaejasmenin B has anticancer and antitumor activity, inhibiting cancer cell migration and invasion, and inhibiting tumor metastasis.Chamaejasmenin B is used in the study of cancers such as breast cancer.

Naxitamab (Hu3F8) is a humanized monoclonal antibody against GD2 (hu3F8). Naxitamab has antitumor activity and can be used to study neuroblastoma, osteosarcoma, and other GD2-positive cancers.

ADT-007 is an orally active and selective pan-RAS inhibitor with potent anticancer activity.ADT-007 blocks GTP activation of RAS and MAPK/AKT signaling by binding to anucleotide RAS.ADT-007 is used in the study of gastrointestinal cancers.

FQI 1 is a selective late-stage SV40 factor (LSF) inhibitor with anticancer activity that exerts its antiproliferative activity by disrupting the mitotic spindle.FQI 1 inhibits the proliferation of NIH/3T3, HeLa, and A549 cells, and can be used in the study of cancers.

JAB-3068 (SHP2-IN-6) is a potent SHP2 inhibitor with anticancer and antitumor activity for the study of breast, lung, and esophageal cancers.

SIC5-6 is a potent inhibitor of Separase, a substantial cysteine protease implicated in critical cellular processes such as chromosome segregation during mitosis and meiosis, DNA damage repair, centrosome disengagement and duplication, as well as spindle stabilization and elongation. Given its overexpression in many solid cancers, Separase presents an attractive target for chemotherapy [1].

VIPhyb is a vasoactive intestinal polypeptide (VIP) receptor antagonist utilized for research in various cancers, including non-small cell lung cancer (NSCLC) [1].

PROTAC SMARCA2 degrader-2, a selective and powerful degrader of SMARCA2/4, exhibits an IC50 of <0.1 μΜ in the HeLa HiBiT assay.this compound holds promise for research into cancers related to or deficient in SMARCA4 [1].

Syk-IN-4 is a potent, selective, and orally bioavailable inhibitor of SYK, demonstrating an IC50 of 0.31 nM. It targets SYK, which has been identified as a potential therapeutic target for autoimmunity and hematological cancers[1].

Calcium N5-methyltetrahydrofolate (NSC-173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers

MP-PEG8-VA-PABC-PBD Dimer is a drug-linker conjugates for ADC which is used in the treatment of several cancers. PBD Dimer is a DNA alkylating which inhibits DNA replication[1].

MRT-14 is a potent Smo antagonist and can be used in several types of cancers linked to abnormal Hh signaling studies.

P3FI-63 is a selective KDM3B inhibitor (IC50: 7 μM) with antitumor activity for the study of fusion-positive rhabdomyosarcoma and other transcriptionally addictive cancers.

MS934, a novel VHL-recruiting MEK 1/2 degrader, exhibits potent anti-proliferative effects on HT-29 cell growth, achieving a GI50 of 0.023 μM. It holds potential for researching various human cancers including melanoma, non-small cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma [1].

Paucimannose, a prevalent mannosidic N-glycoepitope found in invertebrates and plants, is also expressed in cancers [1].

Elisidepsin (PM02734), a cyclic depsipeptide, exhibits antineoplastic activity by inhibiting cancer cell proliferation and is under research for the treatment of various cancers, including non-small cell lung cancer (NSCLC) [1] [2] [3] [4].

4N1K peptide, a biologically active peptide derived from thrombospondins (KRFYVVMWKK), exhibits anti-cancer activities in various cancers.