| DC75305 |
Vandetanib |
Vandetanib is an orally bioavailable 4-anilinoquinazoline. Vandetanib selectively inhibits the tyrosine kinase activity of vascular endothelial growth factor receptor 2 (VEGF2), thereby blocking VEGF-stimulated endothelial cell proliferation and migration and reducing tumor vessel permeability. This agent also blocks the tyrosine kinase activity of epidermal growth factor receptor (EGFR), a receptor tyrosine kinase that mediates tumor cell proliferation and migration and angiogenesis. Vandetanib was the first drug to be approved by FDA (April 2011) for treatment of late-stage (metastatic) medullary thyroid cancer in adult patients who are ineligible for surgery. Vandetanib was approved in 2011. |
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| DC75306 |
BTZ043 Racemic |
BTZ043 Racemic is a mixture of BTZ043-S-isomer and BTZ043-R-isomer. BTZ043 is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor acting as a new antimycobacterial agent that kill Mycobacterium tuberculosis. |
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| DC75307 |
Ruxolitinib free base |
Ruxolitinib, also known as INC424 and INCB18424 or INCB018424, is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies. |
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| DC75308 |
RGX-104 HCl |
RGX-104, also known as SB 742881, is a liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene. |
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| DC75309 |
R-GNE-140 |
R-GNE-140 a novel potent lactate dehydrogenase (LDHA) inhibitor with IC50 3nM for LDHA and 5 nM for LDHB. In MIA PaCa-2 human pancreatic cells, LDHA inhibition rapidly affected global metabolism, although cell death only occurred after 2 d of continuous LDHA inhibition. Pancreatic cell lines that utilize oxidative phosphorylation (OXPHOS) rather than glycolysis were inherently resistant to GNE-140, but could be resensitized to GNE-140 with the OXPHOS inhibitor phenformin. Acquired resistance to GNE-140 was driven by activation of the AMPK-mTOR-S6K signaling pathway, which led to increased OXPHOS, and inhibitors targeting this pathway could prevent resistance. |
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| DC75310 |
p-MPPI HCl |
p-MPPI HCl is a selective 5-HT1A serotonin receptor antagonist, crossing the blood-brain barrier. |
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| DC75311 |
PhTx-74 HCl |
Philanthotoxin-74, also known as PhTx-74, is a synthetic analog of the naturally-occurring wasp venom toxin philanthotoxin-4,3,3. PhTX-74 may be of potential use in studies of the neurobiological role of GluA2-containing subtypes. |
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| DC75312 |
Gefapixant |
Gefapixant, also known as AF-219 or MK-7264, is a P2X3 receptor antagonist. Gefapixant is currently under clinical trials for chronic cough. It is believed that excessive activation of P2X3 receptors is associated with hyper-sensitization of sensory neurons. Neuronal hyper-sensitization in the airways and lungs, triggered by injury or infection, can cause an exaggerated, persistent and frequent urge to cough, so called chronic cough.||P2X3 receptors seem to have a key role in mediation of cough neuronal hypersensitivity. Antagonists of P2X3 receptors such as AF-219 are a promising new group of antitussives. |
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| DC75313 |
Motesanib phosphate |
Motesanib, also known as AMG-706, is the orally bioavailable multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity. Motesanib selectively targets and inhibits vascular endothelial growth factor (VEGFR), platelet-derived growth factor (PDGFR), kit, and Ret receptors, thereby inhibiting angiogenesis and cellular proliferation. |
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| DC75314 |
Copanlisib HCl |
Copanlisib also known as BAY 80-6946, is a potent phosphoinositide 3-kinase (PI3K) inhibitor. Copanlisib inhibits the activation of the PI3K signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Copanlisib was approved for the treatment of adult patients experiencing relapsed follicular lymphoma who have received at least two prior systemic therapies. |
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| DC75315 |
Rucaparib phosphate |
Rucaparib, also known as AG-14699 or PF-01367338, is a tricyclic indole poly(ADP-Ribose) polymerase (PARP1) inhibitor with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Rucaparib selectively binds to PARP1 and inhibits PARP1-mediated DNA repair, thereby enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. |
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| DC75316 |
Pyridostatin TFA salt |
Pyridostatin stabilizes G-quadruplexes (G4s) in cells and elicits a DNA damage response by causing the formation of DNA double strand breaks (DSB). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets gene bodies containing clusters of sequences with a propensity for G-quadruplex formation. As a result, pyridostatin modulated the expression of these genes, including the proto-oncogene SRC. |
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| DC75317 |
NSC23766 3HCl |
NSC23766 is a potent Rac1 inhibitor. NSC23766 disrupted polar secretion of adhesive, polarization of endomembranes, and tip-focused growth in the rhizoid. NSC23766 can acts as a competitive antagonist at muscarinic acetylcholine receptors. NSC23766 exerts anti-influenza virus properties by affecting the viral polymerase complex activity. NSC23766 suppresses CREB signaling by targeting NMDA receptor function. |
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| DC75318 |
Gilteritinib |
Gilteritinib, also known as ASP2215, is a potent FLT3/AXL inhibitor, which showed potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations. In invitro, among the 78 tyrosine kinases tested, ASP2215 inhibited FLT3, LTK, ALK, and AXL kinases by over 50% at 1 nM with an IC50 value of 0.29 nM for FLT3, approximately 800-fold more potent than for c-KIT, the inhibition of which is linked to a potential risk of myelosuppression. ASP2215 inhibited the growth of MV4-11 cells, which harbor FLT3-ITD, with an IC50 value of 0.92 nM, accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6. ASP2215 decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells. ASP2215 may have potential use in treating AML. |
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| DC75319 |
ABP-700 |
ABP-700 is an etomidate analog that is effective as an anesthetic. |
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| 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. |
|
| DC75330 |
PRX-07034 HCl |
PRX-07034 is a selective 5-HT6 receptor antagonist. |
|
| DC75331 |
BMS 182874 |
BMS 182874 is an endothelin receptor antagonist and antihypertensive agent. |
|
| 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). |
|
| 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. |
|
| 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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