VD/VDR- vd-vdr

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Posts by VD/VDR- vd-vdr

AGI-5198 (IDH-C35) is the first highly potent and selective mutant IDH1 inhibitor that was shown to have anti-tumor efficacy and lower tumor 2‑HG (2-hydroxyglutarate) in vivo. It inhibits IDH1 R132H mutant and R132C mutant in vitro with IC50 ~0.07 µM and ~0.16 µM, respectively, but not wild-type IDH1 or any of the examined IDH2 isoforms (IC50 > 100 ¦ÌM). AGI-5198 has good cellular activities in TS603 glioma cell line, also inhibits 2-HG production in HT1080 and U87MG cells with IC50 ~0.48 µM and IC50 ~0.07 µM, respectively. In R132H-IDH1 glioma xenografts (TS603), AGI-5198 (450 mg/kg) caused 50-60% growth inhibition with no signs of toxicity during three weeks of daily treatment, but it did not affect the growth of IDH1 wild-type glioma xenografts (TS516). Under conditions of near complete R-2HG (R-2-hydroxyglutarate) inhibition, AGI-5198 induced demethylation of histone H3K9me3 and expression of genes associated with gliogenic differentiation. Blockade of mutant IDH1 impaired the growth of IDH1-mutant¡ªbut not IDH1-wild-type¡ªglioma cells without appreciable changes in genome-wide DNA methylation. AGI-5198 could serve as a very useful chemical probe to assess the biological consequences of IDH1 mutations and the potential of IDH1 inhibitor for treating IDH1 mutant tumors.

 June 21, 2017

prudect name : AGI-5198 (IDH-C35) is the first highly potent and selective mutant IDH1 inhibitor that was shown to have anti-tumor efficacy and lower tumor 2‑HG (2-hydroxyglutarate) in vivo. It…

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Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective over other serine proteases.

prudect name : Alvelestat (AZD9668) is an oral, highly selective inhibitor of neutrophil elastase (NE) with IC50 and Ki of 12 nM and 9.4 nM, at least 600-fold more selective…

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AG 18; AG 18 (pharmaceutical); RG 50810; RG 50858; TX 825; Tyrphostin 23; Tyrphostin A 23; Tyrphostin AG 18 inhibits EGFR with IC50 of 40 ¦ÌM.

prudect name : AG 18; AG 18 (pharmaceutical); RG 50810; RG 50858; TX 825; Tyrphostin 23; Tyrphostin A 23; Tyrphostin AG 18 inhibits EGFR with IC50 of 40 ¦ÌM.AG 18;…

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prudect name : Ancitabine hydrochlorideSynonyms: (-)-Cyclocytidine hydrochlorideCAS NO: 10212-25-6Molecular Formula: C9H11N3O4.HClMolecular Weight: 261.66Purity: 99%Solubility: Storage:

prudect name : Ancitabine hydrochloride Synonyms: (-)-Cyclocytidine hydrochlorideCAS NO: 10212-25-6Molecular Formula: C9H11N3O4.HClMolecular Weight: 261.66Purity: 99%Solubility: Storage: −20°C 2 years 943962-47-8 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18501888

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prudect name : AminopterinumSynonyms: CAS NO: 54-62-6Molecular Formula: C19H20N8O5Molecular Weight: 440.41Purity: 99%Solubility: Storage: −20°C

prudect name : Aminopterinum Synonyms: CAS NO: 54-62-6Molecular Formula: C19H20N8O5Molecular Weight: 440.41Purity: 99%Solubility: Storage: −20°C 2 years 34157-83-0 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18501737

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ABT-199 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, currently in clinical trials. ABT-199 inhibits the growth of BCL-2-dependent tumors in vivo and spares human platelets. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicate that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2-dependent hematological cancers.

prudect name : ABT-199 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, currently in clinical trials. ABT-199 inhibits the growth of BCL-2-dependent tumors in vivo and…

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A-674563 is achieved from A-443654 by replacing the indole with a phenyl moiety and getting oral activity. A-674563 slows proliferation of tumor cells with EC50 of 0.4 ¦ÌM. A-674563 does not inhibit Akt phosphorylation per se, but blocks the phosphorylation of Akt downstream targets in a dose-dependent manner. A-674563 induced Akt blockade results in decreased STS cell downstream target phosphorylation and tumor cell growth inhibiton. A-674563 induces G2 cell cycle arrest and apoptosis in STS cells.

prudect name : A-674563 is achieved from A-443654 by replacing the indole with a phenyl moiety and getting oral activity. A-674563 slows proliferation of tumor cells with EC50 of 0.4…

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AS-605240 is a PI3K ¦Ã inhibitor (IC50 at 8 nM), which displays 30-fold selectivity over PI3K¦Ä and PI3K¦Â and 7.5-fold selectivity over PI3K¦Á. This agent is the first examples of selective PI3K ¦Ã inhibitors, and was used to block neutrophil chemotaxis in vitro and in vivo. In passive mouse models for rheumatoid arthritis these compounds minimized progression of joint destruction.

prudect name : AS-605240 is a PI3K ¦Ã inhibitor (IC50 at 8 nM), which displays 30-fold selectivity over PI3K¦Ä and PI3K¦Â and 7.5-fold selectivity over PI3K¦Á. This agent is the…

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APY0201 is a potent, highly selective PIKfyve kinase inhibitor.APY0201 exerts its inhibitory activity of IL-12/23 production via PIKfyve inhibition. APY0201 inhibited the conversion of PI3P to PI(3,5)P2 in the presence of recombinant human PIKfyve with an IC50 value of 8.9 nM. It is highly selective for PIKfyve compared to various receptors, channels and enzymes including 25 lipid kinases and 83 protein kinases.APY0201 demonstrated potent in vitro inhibitory activity against interleukin(IL)-12p70 production from mouse macrophages and human PBMCs with an IC50 value of 8.4 nM and 9.9 nM, respectively..For the detailed information of APY-0201, the solubility of APY-0201 in water, the solubility of APY-0201 in DMSO, the solubility of APY-0201 in PBS buffer, the animal experiment (test) of APY-0201, the cell expriment (test) of APY-0201, the in vivo, in vitro and clinical trial test of APY-0201, the EC50, IC50,and affinity,of APY-0201

prudect name : APY0201 is a potent, highly selective PIKfyve kinase inhibitor.APY0201 exerts its inhibitory activity of IL-12/23 production via PIKfyve inhibition. APY0201 inhibited the conversion of PI3P to PI(3,5)P2…

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AdipoRon is a novel small-molecule AdipoR agonist; binds to both AdipoR1(Kd= 1.8 uM) and AdipoR2(Kd=3.1 uM).

prudect name : AdipoRon is a novel small-molecule AdipoR agonist; binds to both AdipoR1(Kd= 1.8 uM) and AdipoR2(Kd=3.1 uM).AdipoRon Synonyms: CAS NO: 924416-43-3Molecular Formula: C27H28N2O3Molecular Weight: 428.52Purity: 98% minSolubility: in…

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