| DC75320 |
Barnidipine HCl |
Barnidipine Hydrochloride is a dihydropyridine calcium channel blocker that has an IC50 value of 0.35 nM in potassium-induced tonic contraction of pig coronary artery. It demonstrates antihypertensive activity by reducing peripheral vascular resistance. It decreases blood pressure in spontaneously hypertensive rats when administered orally at 1 and 3 mg/kg per day. Formulations containing barnidipine have been used in the treatment of hypertension. |
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| DC75321 |
Lorlatinib (PF-06463922) |
Lorlatinib, also known as PF-06463922, is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity. Upon administration, ALK/ROS1 inhibitor PF-06463922 binds to and inhibits both ALK and ROS1 kinases. The kinase inhibition leads to disruption of ALK- and ROS1-mediated signaling and eventually inhibits tumor cell growth in ALK- and ROS1-overexpressing tumor cells. In addition, PF-06463922 is able to cross the blood brain barrier. |
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| DC75322 |
PF-06260933 |
PF-06260933 is a potent and highly selective inhibitor of MAP4K4. |
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| DC75323 |
BMS-863233 HCl |
BMS-863233, also known as XL-413, is an orally bioavailable cell division cycle 7 homolog (CDC7) kinase inhibitor with potential antineoplastic activity. CDC7 kinase inhibitor BMS-863233 binds to and inhibits the activity of CDC7, which may result in the inhibition of DNA replication and mitosis, the induction of tumor cell apoptosis, and the inhibition of tumor cell proliferation in CDC7-overexpressing tumor cells. CDC7, a serine-threonine kinase overexpressed in a variety of tumor cell types, plays an essential role in the initiation of DNA replication by activating origins of replication. |
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| DC75324 |
PX-478 HCl |
PX-478 is an orally active small molecule that inhibits hypoxia-inducible factor 1-alpha (HIF1A) expression, potentially leading to decreased expression of genes important for tumor growth, reduced tumor cell proliferation, and induced apoptosis. Its mechanism of action is independent of VHL and p53 tumor suppressor genes and may involve glucose uptake and metabolism disruption through Glut-1 inhibition. PX-478 demonstrates excellent activity against human tumor xenografts, resulting in tumor regressions and growth delays correlated with HIF-1 levels. |
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| DC75325 |
PSMA-617 TFA |
PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC. |
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| DC75326 |
Selisistat racemate |
Selisistat racemate is a racemic mixture of EX-527, an inhibitor of sirtuin 1 (SIRT1; IC50 = 0.098 µM). It is selective for SIRT1 over SIRT2, and SIRT3 (IC50s = 19.6 and 48.7 µM, respectively) and the cytochrome P450 (CYP) isoforms CYP3A4, CYP2D6, CYP2C9, CYP2C19, and CYP1A2 at 1 µM. EX-527 (50 µM) induces cell cycle arrest at the G1 phase in MCF-7 cells. |
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| DC75327 |
BMS-1001 HCl |
BMS-1001 is a potent PD-1/PD-L1 interaction inhibitor. BMS-1001 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. BMS-1001 is capable of alleviating the PD-1/PD-L1 immune checkpoint-mediated exhaustion of Jurkat T-lymphocytes. |
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| DC75328 |
Plerixafor HCl |
Plerixafor, also known as AMD3100, is a bicyclam with hematopoietic stem cell-mobilizing activity. In the form of its zinc complex, plerixafor acts as an antagonist (or perhaps more accurately a partial agonist) of the alpha chemokine receptor CXCR4 and an allosteric agonist of CXCR7. The CXCR4 alpha-chemokine receptor and one of its ligands, SDF-1, are important in hematopoietic stem cell homing to the bone marrow and in hematopoietic stem cell quiescence. Plerixafor has been found to be a strong inducer of mobilization of hematopoietic stem cells from the bone marrow to the bloodstream as peripheral blood stem cells.[10] Additionally, plerixafor inhibits CD20 expression on B cells by interfering with CXCR4/SDF1 axis that regulates its expression. |
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| DC75329 |
Belfosdil |
Belfosdil, also known as BMY 21891 and SR 7037, is an antihypertensive calcium channel blocker. |
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| DC75330 |
PRX-07034 HCl |
PRX-07034 is a selective 5-HT6 receptor antagonist. |
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| DC75331 |
BMS 182874 |
BMS 182874 is an endothelin receptor antagonist and antihypertensive agent. |
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| DC75332 |
Pixantrone Maleate |
Pixantrone is a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity. Pixantrone is a potentially more effective, less cardiotoxic alternative to doxorubicin for patients with aggressive non-Hodgkin lymphoma (aNHL). |
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| DC75333 |
AZD5991 free acid |
AZD5991 is a potent and selective Mcl-1 inhibitor for treatment of hematologic cancers. AZD5991 is a rationally designed macrocycle with sub-nanomolar affinity for Mcl-1. AZD5991 is an inhibitor of induced myeloid leukemia cell differentiation protein (myeloid cell leukemia-1; Mcl-1; Bcl2-L-3), with potential pro-apoptotic and antineoplastic activities. Upon administration, AZD5991 binds to Mcl-1, thereby preventing the binding of Mcl-1 to and inactivation of certain pro-apoptotic proteins, and promoting apoptosis of cells overexpressing Mcl-1. |
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| DC75334 |
Golotimod |
Golotimod, also known as Orilotimod, SCV-07, is an orally bioavailable synthetic peptide containing the amino acids D-glutamine and L-tryptophan connected by a gamma-glutamyl linkage with potential immunostimulating, antimicrobial and antineoplastic activities. Although the exact mechanism of action is unknown, golotimod appears to inhibit the expression of STAT-3, reversing immunosuppression and stimulating an anti-tumor immune response. This agent may stimulate the production of T-lymphocytes (in particular the helper T [Th1] cells), activate macrophages, and increase levels of interleukin 2 and interferon gamma. STAT-3, a transcription factor upregulated in many cancer cell types, is involved in tumor cell growth and survival and immunosuppression. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus) |
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| DC75335 |
TCS-401 HCl |
TCS-401 (HCI) is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B; Ki = 0.29 µM). It inhibits the protein phosphatases CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1, and LAR D1D2 at much higher concentrations (Kis = 59, 560, 1,100, >2,000, >2,000, and >2,000 μM, respectively).1 Several PTPs have been proposed to act as negative regulators of insulin signaling, thus this enzyme is a potential drug target in diabetes. |
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| DC75336 |
Phosphatidyl choline (from Soybean) |
Phosphatidylcholines (PC) are a class of phospholipids that incorporate choline as a headgroup. They are a major component of biological membranes and can be easily obtained from a variety of readily available sources, such as egg yolk or soybeans, from which they are mechanically or chemically extracted using hexane. They are also a member of the lecithin group of yellow-brownish fatty substances occurring in animal and plant tissues. Dipalmitoyl phosphatidylcholine (aka: lecithin) is a major component of pulmonary surfactant and is often used in the L/S ratio to calculate fetal lung maturity. |
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| DC75337 |
KN-93 (HCI) |
KN-93 is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II). It inhibits fibroblast CaMK-II activity and cell growth in a dose-dependent manner, reversibly arrests cells in G1 and induces apoptosis. |
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| DC75338 |
PF-562271 Besylate |
PF-562271 Besylate, also known as PF-562,271 and PF-271, is an orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. PF-562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival. Note: PF-562271 benzesulfonate is also called PF-562271 besylate. |
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| DC75339 |
Levomefolate calcium |
Levomefolate calcium, also known as LMCA and BAY 86-7660, is the calcium salt of 5-methyltetrahydrofolic acid, a biologically active form of folic acid that functions, in conjunction with Vitamin B12 , as a methyl-group donor involved in the conversion of homocysteine to methionine. Levomefolate is included in formulations of certain oral contraceptives to ensure adequate folic acid levels in women of child-bearing age to reduce the risk of neural tube defects. |
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| DC75340 |
Glasdegib (PF-04449913) |
Glasdegib, also known as PF-04449913, is an orally bioavailable small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. Hedgehog inhibitor PF-04449913 appears to inhibit Hh pathway signaling. The Hh signaling pathway plays an important role in cellular growth, differentiation and repair. Constitutive activation of Hh pathway signaling has been observed in various types of malignancies. |
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| DC75341 |
Gemcitabine Hydrochloride |
Gemcitabine hydrochloride is the hydrochloride salt of an analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis. |
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| DC75342 |
SNS-032 |
SNS-032, also known as BMS-387032, is a 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDK inhibitor SNS-032 selectively binds to CDKs 2, 7, and 9, preventing their phosphorylation and activation; inhibition of CDK activity may result in cell cycle arrest, the induction of apoptosis and decreased tumor cell proliferation in susceptible tumor cell populations. This agent has been shown to sensitize radioresistant tumor cells to ionizing radiation. |
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| DC75343 |
SB-334867 free base |
SB-334867 is an orexin antagonist. It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX1, with around 50x selectivity for OX1 over OX2 receptors. It has been shown to produce sedative and anorectic effects in animals, and has been useful in characterising the orexinergic regulation of brain systems involved with appetite and sleep, as well as other physiological processes. Orexin antagonists have multiple potential clinical applications including the treatment of drug addiction, insomnia, obesity and diabetes. |
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| DC75344 |
Semaglutide |
Semaglutide is a glucagon-like peptide-1 receptor agonist. The drug decreases blood sugar levels. The decrease is theorized to be caused by the mimicking of the incretin glucagon-like peptide-1 (GLP-1). It also appears to enhance growth of pancreatic beta cells, which are responsible for insulin production and release. Additionally, it inhibits the production of glucagon, the hormone that increases glycogenolysis (release of stored carbohydrate from the liver) and gluconeogenesis (synthesis of new glucose). It reduces food intake by lowering appetite and slowing down digestion in the stomach, helping reduce body fat. |
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| DC75345 |
Sitagliptin Phosphate Monohydrate |
Sitagliptin, also known as MK-0431, is a potent inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts. Sitagliptin is believed to exert its actions in patients with type 2 diabetes mellitus by slowing the inactivation of incretin hormones. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. Sitagliptin demonstrates selectivity for DPP-4 and does not inhibit DPP-8 or DPP-9 activity in vitro at concentrations approximating those from therapeutic doses. |
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| DC75346 |
BIBO-3304 TFA |
BIBO-3304 is a selective Y1 receptor antagonist. Y1 receptor proteins from neuropeptide Y have a roll in appetite stimulation. |
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| DC75347 |
Avadomide HCl |
Avadomide, also known as CC-122, is an orally available pleiotropic pathway modulator with potential antineoplastic activity. CC-122 mimics an interferon response and has antitumor activity in DLBCL CC-122 binds Cereblon (CRBN) and promotes degradation of Aiolos and Ikaros in diffuse large B-cell lymphoma (DLBCL) and T cells in vitro, in vivo, and in patients, resulting in both cell autonomous as well as immunostimulatory effects. |
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| DC75348 |
Semaxanib |
Semaxanib, also known as SU5416, is a quinolone derivative with potential antineoplastic activity. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature. This agent also inhibits the phosphorylation of the stem cell factor receptor tyrosine kinase c-kit, often expressed in acute myelogenous leukemia cells. |
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| DC75349 |
Gentamicin sulfate |
Gentamicin is an antibiotic used to treat several types of bacterial infections. This may include bone infections, endocarditis, pelvic inflammatory disease, meningitis, pneumonia, urinary tract infections, and sepsis among others. It is not effective for gonorrhea or chlamydia infections. Gentamicin is a complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1(subA), obtained from Micromonospora purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit protein synthesis. |
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