| DC75103 |
Apatinib free base |
Rivoceranib, also known as Apatinib and YN-968D1, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases. |
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| DC75104 |
Irgacure-651 |
Irgacure 651 is a photoinitiator to enhance the polymer degradation. It was found that the addition of the Irgacure 651 to PMMA accelerated|the photooxidative degradation, particularly at the early stages of exposure. The efficiency of formation of chromophoric groups in PMMA in the presence of the Irgacure initiator was significantly greater than in pure polymer. This suggests that the free-radical products of the initiator photolysis (mainly benzoyl radicals) are able to abstract hydrogen atoms from PMMA molecules. |
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| DC75105 |
Sapanisertib (MLN0128) |
Sapanisertib, also known as TAK-228, MLN0128 and INK128, is a TORC1/2 inhibitor, is an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity. Sapanisertib binds to and inhibits both TORC1 and TORC2 complexes, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation. |
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| DC75106 |
ATC0175 HCl |
ATC0175 is a novel nonpeptidic and orally active melanin-concentrating hormone receptor 1 (MCHR1) antagonist. |
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| DC75107 |
Avadomide free base |
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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| DC75108 |
Axitirome |
Axitirome, also known as CGS26214, is a highly selective thyromimetic and a synthetic cholesterol-lowering agent (HMG CoA reductase inhibitor) shown to be active in the rat, dog and monkey. CGS 26214 is a racemic compound, which is consisted of two equipotent chiral components CGS 28934(-) and CGS 28935(+). CGS 26214, virtually devoid of cardiovascular effects, has potent cholesterol-lowering activity in several models, reduces post-prandial response to a fat load in rats and markedly lowers Lp(a) concentrations in monkeys. |
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| DC75109 |
Fedratinib HCl hydrate |
Fedratinib, also known as TG101348 and SAR302503, is a JAK2 inhibitor, is also an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. JAK2 inhibitor TG101348 competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival. |
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| DC75110 |
Prexasertib HCl |
Prexasertib, also know LY2606368, is a small molecule checkpoint kinase inhibitor that causes DNA double-strand breaks, which results in apoptosis. Prexasertib is mainly active against CHEK1, with minor activity against CHEK2. Preclinical studies have shown that prexasertib induces DNA damage and tumor cell apoptosis in monotherapy. Prexasertib may also potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic agents. |
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| DC75111 |
PF-06651600 free base |
Ritlecitinib, also known as PF-06651600, is a potent and selective JAK3 inhibitor. PF-06651600 is a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies. |
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| DC75112 |
Eleclazine HCl |
Eleclazine HCl is a novel late Na+ current inhibitor. |
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| DC75113 |
Tacrolimus hydrate |
Tacrolimus, also known as FK-506, is an immunosuppressive drug used mainly after allogeneic organ transplant to reduce the activity of the patient's immune system and to lower the risk of organ rejection. It is also used in a topical preparation in the treatment of atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, TH2-mediated diseases such as Kimura's disease, and the skin condition vitiligo. FK-506 is a macrolide isolated from the fungus Streptomyces tsukubaensis. |
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| DC75114 |
Niraparib HCl |
Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway. |
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| DC75115 |
Nicotinamide Riboside Triflate |
Nicotinamide Riboside is a precursor of NAD+ and a source of vitamin B3 (niacin). Nicotinamide Riboside increases intracellular and mitochondrial NAD+ content in C2C12. |
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| DC75116 |
ZEN-2759 |
ZEN-2759 is BRD4(BD1) inhibitor. |
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| DC75117 |
LIT-001 TFA |
LIT-001 is the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. |
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| DC75118 |
Foretinib |
Foretinib, also known as XL880 and GSK1363089, is an orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. |
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| DC75119 |
Ceralasertib |
Ceralasertib, also known as AZD6738, is an orally available morpholino-pyrimidine-based inhibitor of ataxia telangiectasia and rad3 related (ATR) kinase, with potential antineoplastic activity. Upon oral administration, ATR kinase inhibitor Ceralasertib selectively inhibits ATR activity by blocking the downstream phosphorylation of the serine/threonine protein kinase CHK1. This prevents ATR-mediated signaling, and results in the inhibition of DNA damage checkpoint activation, disruption of DNA damage repair, and the induction of tumor cell apoptosis. |
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| DC75120 |
ONO4059-Analog |
ONO4059-Analog, CAS#1351635-67-0, is a potent and selective BTK inhibitor, and is a structural analogue of ONO-4059. ONO4059 is currently under clinical trials. Note: ONO4059 HCl has CAS#1439901-97-9; ONO4059 free base has CAS#1351636-18-4. |
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| DC75121 |
Telaglenastat |
Telaglenastat, also known as CB-839, an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. Telaglenastat selectively and irreversibly inhibits glutaminase. By blocking glutamine utilization, proliferation in rapidly growing cells is impaired. Glutamine-dependent tumors rely on the conversion of exogenous glutamine into glutamate and glutamate metabolites to both provide energy and generate building blocks for the production of macromolecules, which are needed for cellular growth and survival. |
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| DC75122 |
Briciclib |
Briciclib, also known as ON 013105 or ON 014185, is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity. Upon hydrolysis, cyclin D modulator ON 013105 is converted to ON 013100, which blocks cyclin D mRNA translation and decreases protein expression of cyclin D. This may induce cell cycle arrest and apoptosis in cancer cells overexpressing cyclin D and eventually decrease tumor cell proliferation. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents. |
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| DC75123 |
JI-101 free base |
JI-101, also known as CGI-1842, is an orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101 binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so, cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. |
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| DC75124 |
BTZ043 |
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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| DC75125 |
Crenigacestat |
Crenigacestat, also known as LY3039478, is a orally bioavailable, novel small molecule Notch inhibitor with an IC50 of ~1nM in most of the tumor cell lines tested. LY3039478 potently inhibits mutant Notch receptor activity. In a xenograft tumor model, LY3039478 inhibited N1ICD cleavage and expression of Notch-regulated genes in the tumor microenvironment. LY3039478 is being investigated in Phase I. |
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| DC75126 |
Ixazomib citrate |
Ixazomib citrate, also known as MLN9708, is a prodrug of Ixazomib (MMLN-2238). MLN9708 is an orally bioavailable second generation proteasome inhibitor (PI) with potential antineoplastic activity. MLN9708, after hydrolyzing to pharmacologically active MLN2238 (ixazomib), is a next-generation proteasome inhibitor with demonstrated preclinical and clinical antimyeloma activity. MLN9708, compared with bortezomib, has improved pharmacokinetics, pharmacodynamics, and antitumor activity in preclinical studies. |
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| DC75127 |
Asciminib HCl |
Asciminib, also known as ABL001, is a potent allosteric inhibitor of BCR-ABL. ABL001 prevents emergence of resistant disease when administered in combination with nilotinib in an in vivo murine model of chronic myeloid leukemia. Cell proliferation studies demonstrate that ABL001 selectively inhibited the growth of CML and Ph+ ALL cells with potencies ranging from 1-10nM range. ABL001 was tested for activity against clinically observed mutations and found to be active in the low nM range. In the KCL-22 mouse xenograft model, ABL001 displayed potent anti-tumor activity with complete tumor regression observed and a clear dose-dependent correlation with pSTAT5 inhibition. |
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| DC75128 |
Glycovir |
Glycovir, also known as SC-49483, is an anti-HIV prodrug. Glycovir is an alpha-glucosidase-1 inhibitor, and a candidate anti-HIV agent targeted against viral glycoprotein processing in host cell endoplasmic reticulum. |
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| DC75129 |
Bemitradine |
Bemitradine is a diuretic antihypertensive agent. |
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| DC75130 |
Merestinib (LY2801653) |
Merestinib, also known as LY2801653, is an orally available, small molecule inhibitor of the proto-oncogene c-Met (mesenchymal-epithelial transition, also known as hepatocyte growth factor receptor [HGFR]) with potential antineoplastic activity. c-Met inhibitor LY2801653 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. This agent has potent anti-tumor efficacy in mono- and combination therapy in a broad range of cancers. |
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| DC75131 |
Itacitinib |
Itacitinib, also known as INCB39110 or INCB039110, is a potent JAK1 tyrosine kinase inhibitor, which is currently in Phase II trials for the treatment of rheumatoid arthritis, myelofibrosis, rheumatoid arthritis and plaque psoriasis. INCB039110 produced significant improvements in sPGA, demonstrating proof of concept in chronic plaque psoriasis. |
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| DC75132 |
BIIB021 |
BIIB021, also known as CNF2024, is an orally active, purine-scaffold, small-molecule inhibitor of heat shock protein 90 (HSP90) with potential antineoplastic activity. HSP90 inhibitor CNF2024 specifically blocks active HSP90, inhibiting its chaperone function and promoting the degradation of oncogenic signaling proteins involved in tumor cell proliferation and survival; this may result in the inhibition of cellular proliferation in susceptible tumor cell populations. |
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