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Potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). Exhibits up to 1,000 fold selectivity against other TTX-sensitive or resistant sodium channels (IC50 values are >10 ¦ÌM for human NaV1.5 and NaV1.8 channels). Interacts with an inhibitory interaction site distinct from those bound by TTX and local anesthetic-like modulators.

June 21, 2017

prudect name : Potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). Exhibits up to 1,000 fold selectivity against other TTX-sensitive…

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IC-87114 is the first isoform-selective PI3K inhibitor. This quinazolinone purine inhibits p110¦Ä(IC50=0.13µM) at mid-nanomolar concentrations and shows 100¨C1000-fold selectivity over other class I PI3Ks (p110¦Á, p110¦Â and p110¦Ã ). The selectivity of IC87114 is remarkable given that the residues that line the ATP binding pocket of the class I PI3Ks are highly conserved.

prudect name : IC-87114 is the first isoform-selective PI3K inhibitor. This quinazolinone purine inhibits p110¦Ä(IC50=0.13µM) at mid-nanomolar concentrations and shows 100¨C1000-fold selectivity over other class I PI3Ks (p110¦Á, p110¦Â and…

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Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR.

prudect name : Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR…

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3E)-3-(2-Oxo-1H-Indol-3-Ylidene)-1H-Indol-2-One; 3-(2-Oxoindolin-3-Ylidene)Indolin-2-One; (3E)-3-(2-Oxoindolin-3-Ylidene)Indolin-2-One

prudect name : 3E)-3-(2-Oxo-1H-Indol-3-Ylidene)-1H-Indol-2-One; 3-(2-Oxoindolin-3-Ylidene)Indolin-2-One; (3E)-3-(2-Oxoindolin-3-Ylidene)Indolin-2-OneIsoindigotin Synonyms: CAS NO: 476-34-6Molecular Formula: C16H10N2O2Molecular Weight: 262.27Purity: 98% minSolubility: in DMSOStorage: -20oC BMS 817378 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18519784

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prudect name : ImiquimodSynonyms: CAS NO: 99011-02-6Molecular Formula: C14H16N4Molecular Weight: 240.31Purity: 98% minSolubility: Storage: -20°C

prudect name : Imiquimod Synonyms: CAS NO: 99011-02-6Molecular Formula: C14H16N4Molecular Weight: 240.31Purity: 98% minSolubility: Storage: -20°C L 084 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18519747

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Inolitazone is an orally bioavailable PAPR-gamma inhibitor with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction of tumor cell differentiation and apoptosis, and so a reduction in tumor cell proliferation. PPAR-gamma is a nuclear hormone receptor and ligand-activated transcription factor controlling gene expression involved in such cellular processes as differentiation, apoptosis, cell-cycle control, carcinogenesis, and inflammation.

prudect name : Inolitazone is an orally bioavailable PAPR-gamma inhibitor with potential antineoplastic activity. Inolitazone binds to and activates peroxisome proliferation-activated receptor gamma (PPAR-gamma), which may result in the induction…

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prudect name : Isonipecotic acidSynonyms: CAS NO: 498-94-2Molecular Formula: C6H11NO2Molecular Weight: 129.16Purity: 99%Solubility: Storage: −20°C

prudect name : Isonipecotic acid Synonyms: CAS NO: 498-94-2Molecular Formula: C6H11NO2Molecular Weight: 129.16Purity: 99%Solubility: Storage: −20°C 2 years TGR 1202 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18519692

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INNO-206 is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity. Following intravenous administration, doxorubicin prodrug 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.

prudect name : INNO-206 is the 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity. Following intravenous administration, doxorubicin prodrug INNO-206 binds selectively to the cysteine-34…

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Imatinib Mesylate is a multitargeted c-kit, PDGF-R and c-ABL inhibitor with IC50 of 3.9 and 2.9 ¦ÌM for the inhibition of T-cell proliferation stimulated by DCs and PHA, respectively. A reversible tyrosine kinase inhibitor effective in treatment of chronic myelogenous leukemia1 (CML), gastrointestinal stromal tumors, eosinophilic disorders, and systemic mast cell disease. Imatinib Mesylate binds preferentially to ATP¨Cbinding sites of the c-kit protooncogene product, platelet-derived growth factor receptor (PDGF-R), and Abelson kinase (c-ABL) impeding the ensuing signal transduction.

prudect name : Imatinib Mesylate is a multitargeted c-kit, PDGF-R and c-ABL inhibitor with IC50 of 3.9 and 2.9 ¦ÌM for the inhibition of T-cell proliferation stimulated by DCs and…

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idarubicin is a semisynthetic 4-demethoxy analogue of the antineoplastic anthracycline antibiotic daunorubicin. Idarubicin intercalates into DNA and interferes with the activity of topoisomerase II, thereby inhibiting DNA replication, RNA transcription and protein synthesis. Due to its high lipophilicity, idarubicin penetrates cell membranes more efficiently than other anthracycline antibiotic compounds.

prudect name : idarubicin is a semisynthetic 4-demethoxy analogue of the antineoplastic anthracycline antibiotic daunorubicin. Idarubicin intercalates into DNA and interferes with the activity of topoisomerase II, thereby inhibiting DNA…

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