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Riociguat (BAY 63-2521) is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment Phase III clinical trials investigate the use of riociguat as a new approach to treat two forms of pulmonary hypertension (PH): chronic thromboembolic pulmonary hypertension (CTEPH) and pulmonary arterial hypertension (PAH). Riociguat constitutes the first drug of a novel class of sGC stimulators.

June 21, 2017

prudect name : Riociguat (BAY 63-2521) is a novel drug that is currently in clinical development by Bayer. It is a stimulator of soluble guanylate cyclase (sGC). At the moment…

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Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ¡À 8.55 pM)and MT2 (20.1 ¡À 9.25 pM)receptors and selectivity over the MT3 receptor.

prudect name : Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ¡À 8.55 pM)and MT2 (20.1 ¡À 9.25 pM)receptors and selectivity over the…

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RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-_kappa_B.

prudect name : RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-_kappa_B.RTA 408;RTA408 Synonyms: CAS NO: 1474034-05-3Molecular Formula: C33H44F2N2O3Molecular…

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Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.

prudect name : Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.Ruxolitinib (INCB-18424)…

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R547 is a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases with a Ki of median 2 nM for CDK1/cyclin B, CDK2/cyclin E, and CDK4/cyclin D1. In vivo, R547 showed antitumor activity. The selective kinase inhibition profile and the preclinical antitumor activity of R547 suggest that it may be promising for development for use in the treatment of solid tumors. The cyclin-dependent protein kinases are key regulators of cell cycle progression. Aberrant expression or altered activity of distinct cyclin-dependent kinase (CDK) complexes leads to escape of cells from cell cycle control, leading to unrestricted cell proliferation. CDK inhibitors have the potential to induce cell cycle arrest and apoptosis in cancer cells, and identifying small-molecule CDK inhibitors has been a major focus in cancer research. In cell-free assays, R547 was inactive (K(i) > 5,000 nM) against a panel of >120 unrelated kinases. In vitro, R547 effectively prevented the proliferation of tumor cell lines independent of multidrug resistant status, histologic type, retinoblastoma protein, or p53 status, with IC50 < 0.60 ¦ÌM.

prudect name : R547 is a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases with a Ki of median 2 nM for CDK1/cyclin B, CDK2/cyclin E, and…

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RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively.

prudect name : RO5126766 (CH5126766) is a dual RAF/MEK inhibitor with IC50 of 8.2 nM,19 nM, 56 nM, and 160 nM for BRAF V600E, BRAF, CRAF, and MEK1, respectively.RO5126766 Synonyms:…

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prudect name : QuinestrolSynonyms: CAS NO: 152-43-2Molecular Formula: C25H32O2Molecular Weight: 364.53Purity: 98% minSolubility: Storage: −20°C

prudect name : Quinestrol Synonyms: CAS NO: 152-43-2Molecular Formula: C25H32O2Molecular Weight: 364.53Purity: 98% minSolubility: Storage: −20°C web site: www.medchemexpress.com

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prudect name : QS 11Synonyms: CAS NO: 944328-88-5Molecular Formula: C36H33N5O2 Molecular Weight: 567.68Purity: 98% minSolubility:

prudect name : QS 11 Synonyms: CAS NO: 944328-88-5Molecular Formula: C36H33N5O2 Molecular Weight: 567.68Purity: 98% minSolubility: In DMSOStorage: -20°C web site: www.medchemexpress.com

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Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.

prudect name : Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs…

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AC220 (AC 220, AC220) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ¡À 0.3 nM and >10 mM for MC4-11 and A375, respectively. AC220 (AC 220, AC220) exhibits low nanomolar potency in biochemical and cellular assays and exceptional kinase selectivity, and in animal models is efficacious at doses as low as 1 mg/kg given orally once daily. The data reveal that the combination of excellent potency, selectivity, and pharmacokinetic properties is unique to AC220 (AC 220, AC220), which therefore is the first candidate with a profile that matches the characteristics desirable for a clinical FLT3 inhibitor.

prudect name : AC220 (AC 220, AC220) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ¡À 0.3 nM and >10 mM for MC4-11 and A375, respectively….

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