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Chemical Name:(R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone mesylate

June 21, 2017

prudect name : Chemical Name:(R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone mesylateWIN 55212-2 mesylate Synonyms: CAS NO: 131543-23-2Molecular Formula: C27H26N2O3.CH3SO3HMolecular Weight: 522.61Purity: 98% minSolubility: In DMSOStorage: −20°C web site: www.medchemexpress.com

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Biological Activity:JAK3 inhibitor (IC50 = 1.8 ¦ÌM) that displays no activity at JAK1 or JAK2. Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro. Also inhibits other common kinases including EGFR (IC50 = 4 nM), Src, Abl, VEGFR, MAPK and PI 3-K and induces apoptosis in human glioblastoma cell lines (IC50 = 158 ¦ÌM).

prudect name : Biological Activity:JAK3 inhibitor (IC50 = 1.8 ¦ÌM) that displays no activity at JAK1 or JAK2. Inhibits STAT1 activation, iNOS expression and NO production in macrophages in vitro….

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Wortmannin inhibits peritoneal metastasis of SW1990 in mice at 1 mg/kg, without any weight loss. Wortmannin inhibits phosphatidylinositide 3-kinase-protein kinase B (PKB)/Akt phosphorylation in both normal tissues (lung, heart and brain homogenates) and tumor tissue in mice, without mortality or acute toxicity at 0.7 mg/kg. Combination with LY188011, Wortmannin significantly increases apoptosis and inhibit tumor growth in orthotopic tumor, while both monotherapy could not.

prudect name : Wortmannin inhibits peritoneal metastasis of SW1990 in mice at 1 mg/kg, without any weight loss. Wortmannin inhibits phosphatidylinositide 3-kinase-protein kinase B (PKB)/Akt phosphorylation in both normal tissues…

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WAY-362450 binds to the ligand-binding domain (LBD) of human FXR. WAY-362450 resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450. WAY-362450 promotes transcription of the human BSEP, human SHP, and mouse IBABP genes utilizing reporter constructs with EC50 of 17, 230, and 33 nM, respectively in promoter assays. WAY-362450 at concentration of 1 ¦ÌM significantly induces mRNAs encoding for BSEP, SHP, and IBABP in human cell cultures to 13-, 2-, and 20-fold, respectively. WAY-362450 at concentration of 1 ¦ÌM suppresses interleukin-6-induced CRP expression in human Hep3B hepatoma cells, and the inhibitory effect is attenuated when knockdown of FXR by short interfering RNA.

prudect name : WAY-362450 binds to the ligand-binding domain (LBD) of human FXR. WAY-362450 resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450….

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VX-680 gives rise to a marked decrease in tumor size in a human AML (HL-60) xenograft model. In mude mice treateed with VX-680 at 75 mg/kg, twice a day intraperitoneally (b.i.d. i.p.) for 13 days, mean tumor volumes are reduced by 98%. Tumor growth decrease is dose dependent and significant at a dose of 12.5 mg/kg b.i.d. VX-680 is well tolerated, with a small decrease in body weight observed only at the highest dose. VX-680 also triggers tumor regresson in pancreatic and colon xenograft models. VX-680 also displays potent antitumor activity when infused i.v. in mude rats bearing established HCT116 tumors. A higher dose of VX-680 (2 mg/kg/h) improves efficacy with a 56% decrease in mean tumor volume.

prudect name : VX-680 gives rise to a marked decrease in tumor size in a human AML (HL-60) xenograft model. In mude mice treateed with VX-680 at 75 mg/kg, twice…

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USP Standard

prudect name : USP StandardValrubicin Synonyms: CAS NO: 56124-62-0Molecular Formula: C34H36F3NO13Molecular Weight: 723.64 Purity: 98%Solubility: Storage: -20°C web site: www.medchemexpress.com

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prudect name : VX 770Synonyms: CAS NO: 873054-44-5Molecular Formula: C24H28N2O3Molecular Weight: 392.49Purity: 98% minSolubility: In

prudect name : VX 770 Synonyms: CAS NO: 873054-44-5Molecular Formula: C24H28N2O3Molecular Weight: 392.49Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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Voxtalisib, also known as XL-765 and SAR245409, is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR dual kinase inhibitor XL765 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in susceptible tumor cell populations. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion in response to nutrient and energy deprivation. Accordingly, this agent maybe more potent compared to an agent that inhibits either PI3K kinase or mTOR kinase alone.

prudect name : Voxtalisib, also known as XL-765 and SAR245409, is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and…

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prudect name : VilazodoneSynonyms: CAS NO: 163521-12-8Molecular Formula: C26H27N5O2Molecular Weight: 441.52Purity: 98% minSolubility: In DMSOStorage:

prudect name : Vilazodone Synonyms: CAS NO: 163521-12-8Molecular Formula: C26H27N5O2Molecular Weight: 441.52Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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GS-9451 is a potent macrocyclic HCV NS3 PI that achieved a median maximal change in HCV RNA of 3.6 log10 IU/mL (range, -4.7 log10 to -3.1 log10 IU/mL) following 3-day monotherapy in treatment-naïve patients with HCV genotype 1 infection during phase I. In multiple GT1a and GT1b replicon cell lines, GS-9451 had mean 50% effective concentrations (EC50s) of 13 and 5.4 nM, respectively, with minimal cytotoxicity; similar potency was observed in chimeric replicons encoding the NS3 protease gene of GT1 clinical isolates. GS-9451 was less active in GT2a replicon cells (EC50 = 316 nM). GS-9451 showed good oral bioavailability in all three species tested.

prudect name : GS-9451 is a potent macrocyclic HCV NS3 PI that achieved a median maximal change in HCV RNA of 3.6 log10 IU/mL (range, -4.7 log10 to -3.1 log10…

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