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Biological Activity of TAE684: TAE684 is a highly potent and selective smallmolecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM. NVP-TAE684 treatment resulted in a rapid and sustained inhibition of phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest.

June 21, 2017

prudect name : Biological Activity of TAE684: TAE684 is a highly potent and selective smallmolecule ALK inhibitor, which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values…

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Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-¦Á-induced necroptosis with EC50 of 490 nM.

prudect name : Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-¦Á-induced necroptosis with EC50 of 490 nM.Necrostatin-1 Synonyms: CAS NO: 4311-88-0Molecular Formula: C13H13N3OSMolecular Weight: 259.33Purity: 98% minSolubility: in DMSOStorage:…

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NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM. IC50 value: 500 nM (Ki)

prudect name : NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM. IC50 value: 500 nM (Ki)NQDI-1;NQDI1 Synonyms: CAS NO: 175026-96-7Molecular Formula: C19H13NO4Molecular Weight: 319.31Purity: 98%…

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Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.[1] Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. Neratinib also inhibits the epidermal growth factor receptor (EGFR) kinase and the proliferation of EGFR-dependent cells.

prudect name : Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.[1] Neratinib binds to the HER-2…

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LDE225 (NVP-LDE225) is a novel and specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM. It has been shown to potentially inhibit Hh-and Smo-dependent proliferation in vivo. It also induced the regression of preformed basaloid lesions with an IC50 of <150 nmol/l and almost complete regression at 1.5 ¦Ìmol/l. Topical application of a 1% LDE225 (NVP-LDE225) solution to depilated skin of C57/BL6 mice completely inhibited hair growth during anagen phase as well as the expression of the Hh-pathway target genes (Gli1, Gli2, Sox9, and N-Myc) and partial inhibition was obtained when applying a 0.3% solution.

prudect name : LDE225 (NVP-LDE225) is a novel and specific, orally bioavailable Smo inhibitor with an IC50 of 11 nM. It has been shown to potentially inhibit Hh-and Smo-dependent proliferation…

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NVP-BEP800 is a novel, fully synthetic HSP90¦Â inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1

prudect name : NVP-BEP800 is a novel, fully synthetic HSP90¦Â inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1NVP-BEP800 Synonyms: CAS NO: 847559-80-2Molecular Formula:…

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NLG919 potently blocks IDO-induced T-cell suppression and restored robust T-cell responses with ED50 of 80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated IDO-induced suppression of antigen-specific T cells (OT-I) in vitro, with ED50 of 120 nM. In mice, a single oral administration of NLG919 reduces the concentration of plasma and tissue Kyn by ~ 50%. In mice bearing B16F10 tumors, NLG919 markedly enhances the antitumor responses of naive, resting pmel-1 cells to vaccination with cognate hgp100 peptide plus CpG-1826 in IFA.

prudect name : NLG919 potently blocks IDO-induced T-cell suppression and restored robust T-cell responses with ED50 of 80 nM. Similarly, using IDO-expressing mouse DCs from tumor-draining lymph nodes, NLG919 abrogated…

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Nimorazole is a nitroimidazole anti-infective.

prudect name : Nimorazole is a nitroimidazole anti-infective.Nimorazole Synonyms: CAS NO: 6506-37-2Molecular Formula: C9H14N4O3Molecular Weight: 226.23Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18534289

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Afatinib intermediates

prudect name : Afatinib intermediatesN4-(3-Chloro-4-fluorophenyl)-7-[[(3S)-tetrahydro-3-furanyl]oxy]-4,6-quinazolinediamine Synonyms: CAS NO: 314771-76-1Molecular Formula: C18H16ClFN4O2Molecular Weight: 374.80Purity: 98% minSolubility: Storage: -20oC web site: www.medchemexpress.com References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18534287

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Phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT. The stem cell factor (SCF) receptor, KIT, also called CD117 or c-KIT receptor, is a member of the type III receptor protein-tyrosine kinase family (RTK). KIT regulate erythropoiesis, lymphopoiesis, megakaryopoiesis, gametogenesis, melanogenesis, with SCF also serving as an important growth factor. gain-of-function mutations in KIT, that is mutations that cause constitutive activation of the tyrosine kinase (TK), have been implicated in a variety of neoplasms including, gastrointestinal stromal tumours (GIST), mastocytosis, acute leukaemias, melanomas and other cancers.In Ba/F3 cells expressing human wildtype KIT, masitinib dose-dependently inhibited SCF-induced cell proliferation with an IC50 of 150 nM.

prudect name : Phenylaminothiazole-type tyrosine kinase inhibitor that targets KIT. The stem cell factor (SCF) receptor, KIT, also called CD117 or c-KIT receptor, is a member of the type III…

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