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Cat. No.	Product Name	Field of Application
DC75439	Molibresib	Molibresib, also known GSK525762A, I-BET-762 and GSK525762 , is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor GSK525762 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth.
DC75440	Panobinostat	Panobinostat, also known as NVP LBH-589 or LBH-589, is a cinnamic hydroxamic acid analogue with potential antineoplastic activity. Panobinostat selectively inhibits histone deacetylase (HDAC), inducing hyperacetylation of core histone proteins, which may result in modulation of cell cycle protein expression, cell cycle arrest in the G2/M phase and apoptosis. In addition, this agent appears to modulate the expression of angiogenesis-related genes, such as hypoxia-inducible factor-1alpha (HIF-1a) and vascular endothelial growth factor (VEGF), thus impairing endothelial cell chemotaxis and invasion. On 2/23/2015, it received FDA accelerated approval for use in patients with multiple myeloma who had received at least 2 previous treatments, including bortezomib and an immunomodulatory agent.
DC75442	Tenofovir alafenamide fumarate (1:1 salt)	Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1.
DC75443	Belotecan Hydrochloride	Belotecan, also known as CKD-602, is the semi-synthetic camptothecin analogue belotecan with potential antitumor activity. Belotecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the top technicaloisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Topoisomerase I is an enzyme that mediates reversible single-strand breaks in DNA during DNA replication.
DC75444	Spebrutinib	Spebrutinib, also known as AVL-292 or CC-292, is an orally bioavailable, selective inhibitor of BrutonÂ’s agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, AVL-292 targets and covalently binds to BTK, thereby preventing its activity. By irreversibly inhibiting BTK, administration of this agent may lead to an inhibition of B cell receptor (BCR) signaling and may inhibit cell proliferation of B-cell malignancies.
DC75445	Abiraterone	Abiraterone, also known as CB7598, is the active metabolite of abiraterone acetate, which is an orally active acetate ester of the steroidal compound abiraterone with antiandrogen activity. Abiraterone acetate was approved by the U.S. Food and Drug Administration (FDA) in April 2011. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels.
DC75446	Camptothecin	Camptothecin (CPT) is a cytotoxic quinoline alkaloid which inhibits the DNA enzyme topoisomerase I (topo I). It was discovered in 1966 by M. E. Wall and M. C. Wani in systematic screening of natural products for anticancer drugs. It was isolated from the bark and stem of Camptotheca acuminata (Camptotheca, Happy tree), a tree native to China used as a cancer treatment in Traditional Chinese Medicine. CPT showed remarkable anticancer activity in preliminary clinical trials but also low solubility and (high) adverse drug reaction. Because of these disadvantages synthetic and medicinal chemists have developed numerous syntheses of Camptothecin and various derivatives to increase the benefits of the chemical, with good results. Two CPT analogues have been approved and are used in cancer chemotherapy today, topotecan and irinotecan.
DC75447	ATN-161 free base	ATN-161 is a small peptide antagonist of integrin alpha5beta1 with potential antineoplastic activity. ATN-161 selectively binds to and blocks the receptor for integrin alpha5beta1, thereby preventing integrin alpha5beta1 binding. This receptor blockade may result in inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, angiogenesis, and tumor progression. Integrin alpha5beta1 is expressed on endothelial cells and plays a crucial role in endothelial cell adhesion and migration.
DC75448	Fludarabine	Fludarabine is an adenosine analong, DNA chain terminator, and inhibitor of ribonucleotide reductase, DNA ligase, DNA primase, and adenoside A1 receptors. It is use to treat leukemias and graft-versus host disease in transplant patients. It also induces cell cycle arrest and apoptosis in alloreactive bone marrow stromal cells.
DC75449	Galunisertib	Galunisertib, also known as LY2157299, is a novel, selective small molecule transforming growth factor beta receptor (TGF-βR) kinase inhibitor. LY2157299 inhibited HCC cell migration on Laminin-5, Fibronectin, Vitronectin, Fibrinogen and Collagen-I and de novo phosphorylation of pSMAD2. LY2157299 inhibited HCC migration and cell growth independently of the expression levels of TGF-βRII.
DC75451	Nilotinib HCl hydrate	Nilotinib, also known as AMN-107, is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs).
DC75453	Doxorubicin free base	Doxorubicin free base, also called doxorubicin, is an anthracycline antibiotic with antineoplastic activity. Approved API for cancer therapeutic use is doxorubicin HCl. Doxorubicin, isolated from the bacterium Streptomyces peucetius var. caesius, is the hydroxylated congener of daunorubicin. Doxorubicin intercalates between base pairs in the DNA helix, thereby preventing DNA replication and ultimately inhibiting protein synthesis. Note: Doxorubicin free base has low solubility in common solvents. The MedKoo original CAT# for this product was 100280a.
DC75454	Desmopressin acetate trihydrate	Desmopressin acetate is a synthetic replacement for vasopressin, the hormone that reduces urine production. It may be taken nasally, intravenously, or as a tablet. Doctors prescribe Desmopressin most frequently for treatment of diabetes insipidus or nocturnal enuresis. Desmopressin (1-desamino-8-D-arginine vasopressin) is a modified form of the normal human hormone arginine vasopressin, a peptide containing nine amino acids. Medical use of Desmopressin acetate includes: (a) bed wetting; (b) nighttime urination; (c) clotting disorders; (d) diabetes insipidus.
DC75455	XE991 free base	XE991, also known as LS190926, is a potent and selective KCNQ channel blocker. XE991 blocks KCNQ2+3/M-currents (IC50 = 0.6-0.98 μM) and KCNQ1 homomeric channels (IC50 = 0.75 μM) but is less potent against KCNQ1/minK channels (IC50 = 11.1 μM).
DC75456	Aminolevulinic Acid HCl	Aminolevulinic acid, also known as ALA, is a topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid (ALA) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect. In 1999, FDA approved this drug for for actinic keratosis.
DC75457	Abiraterone Acetate	Abiraterone acetate is an FDA approved drug, and is an orally active acetate ester of the steroidal compound abiraterone with antiandrogen activity. Abiraterone acetate was approved by the U.S. Food and Drug Administration (FDA) in April 2011. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels. FDA Approval this drug in May 2011.
DC75460	Palbociclib HCl	Palbociclib, also known as PD0332991, is an orally active, selective inhibitor of the cyclin D kinases Cdk4 (IC50 = 11 nM) and Cdk6 (IC50= 16 nM) with no activity against a panel of 36 additional protein kinases. It has been reported to have antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest at nanomolar concentrations.
DC75462	Lerociclib	Lerociclib , also known as G1T38, is an oral, potent and selective CDK4/6 inhibitor for the treatment of Rb competent tumors. Biochemical profiling demonstrates G1T38 is a competitive, nanomolar inhibitor of CDK4/6 with highly selectivity for CDK4-cyclin D1 and CDK6-cyclin D3. G1T38 exhibits a low EC50 (<100 nM) in Rb competent cell lines compared to >3 μM in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models.
DC75463	K-7174-2HCl	K-7174 is a novel orally active, potent proteasome inhibitor. K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. K-7174 kills bortezomib-resistant myeloma cells carrying a β5-subunit mutation in vivo and primary cells from a patient resistant to bortezomib. K-7174 is also a GATA-specific inhibitor, which may have potential application in treating anemia of chronic disease.
DC75464	Enarodustat	Enarodustat, also known as JTZ-951, is a prolyl hydroxylase inhibitor. JTZ-951 (enarodustat) stabilizes HIF-α protein and induces erythropoiesis without effects on the function of vascular endothelial growth factor. Enarodustat increases endogenous erythropoietin levels in the treatment of anemia associated with chronic kidney disease (CKD). JTZ-951 induces erythropoiesis without affecting VEGF function. JTZ-951 may be a new oral candidate that increases and maintains hemoglobin concentrations in renal anemia patients.
DC75465	Rupitasertib free base	Rupitasertib, also known as M2698, MSC-2363318A, is a potent dual-inhibitor of p70S6K and Akt that affects tumor growth in mouse models of cancer and crosses the blood-brain barrier. M2698 was highly potent in vitro (IC50 1 nM for p70S6K, Akt1 and Akt3 inhibition; IC50 17 nM for pGSK3β indirect inhibition) and in vivo (IC50 15 nM for pS6 indirect inhibition), and relatively selective (only 6/264 kinases had an IC50 within 10-fold of p70S6K).
DC75467	Aldoxorubicin HCl	Aldoxorubicin, also known as INNO-206 and Doxo-EMCH, is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin with antineoplastic activity. INNO-206 binds selectively to the cysteine-34 position of albumin via its maleimide moiety. Doxorubicin is released from the albumin carrier after cleavage of the acid-sensitive hydrazone linker within the acidic environment of tumors and, once located intracellularly, intercalates DNA, inhibits DNA synthesis, and induces apoptosis. Albumin tends to accumulate in solid tumors as a result of high metabolic turnover, rapid angiogenesis, hyervasculature, and impaired lymphatic drainage. Because of passive accumulation within tumors, this agent may improve the therapeutic effects of doxorubicin while minimizing systemic toxicity. NOTE: Current batch has ~90% purity by HPLC. The rest 10% is doxouribin HCl.
DC75468	GW438014 free base	GW438014A is a selective NPY-Y5 receptor antagonist.
DC75470	Desvenlafaxine Succinate hydrate	Desvenlafaxine Succinate is a venlafaxine metabolite and inhibitor of SERT and NET used to treat depression. It also alters rates of gastric emptying and decreases symptoms of menopausal hot flashes.
DC75471	Norepinephrine bitartrate hydrate	Norepinephrine is an organic chemical in the catecholamine family that functions in the human brain and body as a hormone and neurotransmitter. Norepinephrine directly stimulates adrenergic receptors. Stimulation of alpha-adrenergic receptors causes vasoconstriction of the radial smooth muscle of the iris, arteries, arterioles, veins, urinary bladder, and the sphincter of the gastrointestinal tract. Stimulation of beta-1 adrenergic receptors causes an increase in myocardial contractility, heart rate, automaticity, and atrioventricular (AV) conduction while stimulation of beta-2 adrenergic receptors causes bronchiolar and vascular smooth muscle dilatation.
DC75472	Indinavir sulfate	Indinavir sulfate is an inhibitor of HIV protease, GLUT4, and calpain used to treat HIV infection. It also decreases phosphorylation of the insulin receptor β subunit, inhibits adenocarcinoma tumor growth, and may induce SOCS1 signaling.
DC75473	R-IMPP	R-IMPP is an inhibitor of PCSK9 translation. R-IMPP stimulates uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin.
DC75474	Necrosulfonamide	Necrosulfonamide is a novel inhibitor of MLKL (mixed lineage kinase domain-like). Necrosulfonamide is a cell-permeable inhibitor that covalently modifies Cys88 and blocks human MLKL adaptor function. Necrosulfonamide Attenuates Spinal Cord Injury via Necroptosis Inhibition.
DC75475	Saccharin 1-methylimidazole	Saccharin 1-methylimidazole, also known as SMI, is a chemical activator commonly used in solid-phase synthesis of DNA and RNA oligonucleotides. Saccharin 1-methylimidazole has been used to synthesize single-stranded DNA oligonucleotides that are resistant to nuclease digestion.
DC75476	Batimastat	Batimastat (also known as BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Matrix metalloproteinases (MMPs) are thought to play a significant role in tumor invasion and metastasis as well as angiogenesis. Batimastat, also known as BB-94, acts as an inhibitor of metalloproteinase activity by binding the zinc ion in the active site of MMPs.

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