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prudect name : Baricitinib INCB 028050 LY3009104Synonyms: Baricitinib INCB 028050 LY3009104CAS NO: 1187594-09-7Molecular Formula: C16H17N7O2SMolecular

June 21, 2017

prudect name : Baricitinib INCB 028050 LY3009104 Synonyms: Baricitinib INCB 028050 LY3009104CAS NO: 1187594-09-7Molecular Formula: C16H17N7O2SMolecular Weight: 371.42Purity: 98% minSolubility: In DMSOStorage: -20°C 606143-89-9 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18503093

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BMS-794833,a potent ATPcompetitive Met/VEGFR-2 kinase inhibitor,demonstrates enhanced activity versus both Met-dependent and Met-insensitive tumor lines. BMS-794833 also inhibits Ron (Met family),Axl (phylogenetically related Axl/Tyro3/Mer subfamily) and Flt-3 with IC50 values <3 nM. The compound was selective versus a panel of >200 additional RTKs, non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. In cell culture, BMS-794833 inhibited the proliferation of human tumor cell lines containing constitutively activated Met receptor (GTL-16 gastric carcinoma). Tumor cell lines whose growth is stimulated by HGF (U87 glioblastoma) were also effectively inhibited by BMS-794833. In vivo, BMS-794833 demonstrated dose-dependent tumor growth inhibition following oral administration in the GTL-16 and L2987 lung carcinoma (Met-insensitive) xenograft models. Despite the impressive antitumor activity, BMS-794833 showed dissolution rate-limited absorption from solid dosage forms.

prudect name : BMS-794833,a potent ATPcompetitive Met/VEGFR-2 kinase inhibitor,demonstrates enhanced activity versus both Met-dependent and Met-insensitive tumor lines. BMS-794833 also inhibits Ron (Met family),Axl (phylogenetically related Axl/Tyro3/Mer subfamily) and Flt-3…

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BMS-582664 inhibits VEGF-stimulated and FGF-stimulated proliferating of HUVECs with IC50 of 40 nM and 276 nM. BMS-582664 (2 ¦ÌM) significantly inhibits VEGFR2, FGFR1, ERK1/2 and Akt phosphorylation in VEGF- and bFGF-stimulated SK-HEP1 cells and HepG-2 cells, while BMS-582664 alone has little effect on levels of phosphorylated ERK1/2, Akt, VEGFR2, and FGFR1 in nonstimulated cells. BMS-582664 inhibits CYP2C19, CYP3A4(BFC) and CYP3A4 (BzRes) with IC50 of 2.4 ¦ÌM, 0.51 ¦ÌM and 1.6 ¦ÌM, respectively. BMS-582664 exhibits high solid state stability (only 0.3% degradation at 50¡æ with desiccant over a period of 12 weeks) and acceptable solution state stability up to pH 6.5.

prudect name : BMS-582664 inhibits VEGF-stimulated and FGF-stimulated proliferating of HUVECs with IC50 of 40 nM and 276 nM. BMS-582664 (2 ¦ÌM) significantly inhibits VEGFR2, FGFR1, ERK1/2 and Akt phosphorylation…

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Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity. As a SMAC mimetic and IAP antagonist, TL32711 binds to and inhibits the activity of IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains.

prudect name : Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis…

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ATP citrate lyase (ACL) inhibitor (IC50 = 0.13 ¦ÌM for human recombinant ACL); blocks lipid synthesis (IC50 = 8 ¦ÌM in HepG2 cells). Displays no cytotoxicity up to a concentration of 50 ¦ÌM. Lowers plasma glucose and triglycerides in a mouse model of hyperlipidemia. Orally bioavailable.

prudect name : ATP citrate lyase (ACL) inhibitor (IC50 = 0.13 ¦ÌM for human recombinant ACL); blocks lipid synthesis (IC50 = 8 ¦ÌM in HepG2 cells). Displays no cytotoxicity up…

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Tubulin polymerization inhibitors, anti-angiogenic cancer drugs

prudect name : Tubulin polymerization inhibitors, anti-angiogenic cancer drugsBNC105P Synonyms: CAS NO: 945771-96-0Molecular Formula: C20H19Na2O10PMolecular Weight: 496.31Purity: 98% minSolubility: In DMSOStorage: -20°C 1005491-05-3 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18502996

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Belinostat (PXD101) is a novel hydroxamate-type inhibitor of histone deacetylase (HDAC) activity. Belinostat inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM. PXD101 is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range of 0.2-3.4 uM as determined by a clonogenic assay and induces apoptosis.

prudect name : Belinostat (PXD101) is a novel hydroxamate-type inhibitor of histone deacetylase (HDAC) activity. Belinostat inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM. PXD101…

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BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190 reduces the basal levels of inositol phosphate production in cells expressing the CB2 BML-190 is an aminoalkylindole. BML-190 is found to yield at least 15 metabolic products.BML-190 diminishes LPS-induced NO and IL-6 production in a concentration-dependent manner. BML-190 also inhibits LPS-induced PGE2 production and COX-2 induction.

prudect name : BML-190 has 50-fold selectivity for CB2 receptors over CB1 receptors. In HEK-293 cells stably expressing the human CB2 receptor, BML-190 potentiates the forskolin-stimulated accumulation of cAMP. BML-190…

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AG 490 is a potent epidermal growth factor receptor kinase autophosphorylation inhibitor with an IC50 of 100 nM and 56.8¦ÌM for EGFR and JAK, respectively. It inhibits cytokine-independent cell growth in vitro and tumor cell invasion in vivo. It selectively blocks leukemic cell growth in vitro and in vivo by inducing programmed cell death, with no harmful effect on normal hematopoiesis. It inhibits the constitutive activation of STAT-3 DNA binding and IL-2-induced growth of MF tumor cells. It displays apoptotic and antiproliferative properties with IC50 of 1.7, 2.8 and 6.1 µM in 2E8, Baf/3 and Jurkat cells, respectively.

prudect name : AG 490 is a potent epidermal growth factor receptor kinase autophosphorylation inhibitor with an IC50 of 100 nM and 56.8¦ÌM for EGFR and JAK, respectively. It inhibits…

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AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor with an IC50 of 35 nM. AZ3146 efficiently prevented autophosphorylation of full-length Mps1 immunoprecipitated from human cells. AZ 3146 revealed selectivity over 46 other kinases including Cdk1 and aurora kinase B. AZ 3146 is thought to act by interfering with chromosome alignment and overriding the spindle assembly checkpoint. Furthermore, AZ 3146 prevented the recruitment of Mad1, Mad2 and centromere protein E (CENP-E) to kinetochores. AZ3146 also silenced an already established SAC signal; after release from a nocodazole block, AZ3146 dramatically accelerated mitotic exit. Significantly, although Mad1 was present at kinetochores in controls, kinetochores in cells treated with nocodazole plus AZ3146 were devoid of Mad1. AZ 3146 prevented kinetochore localization of Mad2 regardless of the experimental regimen.

prudect name : AZ 3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor with an IC50 of 35 nM. AZ3146 efficiently prevented autophosphorylation of full-length Mps1 immunoprecipitated…

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