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QNZ (EVP4593) is a useful tool to explore the role of NF-¦ÊB in cellular signaling pathways. QNZ also inhibits TNF¦Á production from lipopolysaccharide-stimulated mouse splenocytes with an IC50 of 7 nM.

June 21, 2017

prudect name : QNZ (EVP4593) is a useful tool to explore the role of NF-¦ÊB in cellular signaling pathways. QNZ also inhibits TNF¦Á production from lipopolysaccharide-stimulated mouse splenocytes with an…

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PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ¡À 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ¡À 1.4 nmol/L in cells. This Smo antagonist showed robust antitumor activity in a mouse model of medulloblastoma with an in vivo IC(50) of 8.9 ¡À 2.6 nmol/L. The downregulation of Gli1 is closely linked to the tumor growth inhibition in patched(+/-) medulloblastoma mice. Mathematical analysis of the relationship between the drug¡¯s pharmacokinetics and Gli1 pharmacodynamics in patched(+/-) medulloblastoma tumor models yielded similar tumor and skin Gli1 IC(50) values, suggesting that skin can be used as a surrogate tissue for the measurement of tumor Gli1 levels. In addition, PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. The brain permeability of PF-5274857 was also confirmed and quantified in nontumor-bearing preclinical species with an intact blood-brain barrier. PF-5274857 was orally available and metabolically stable in vivo. These findings suggest that PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.

prudect name : PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ¡À 1.1 nmol/L and completely blocks the transcriptional activity of the…

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AP24534 is a novel potent, orally available small molecule multitargeted kinase inhibitor with IC50 of 0.37, 2, 1.5, 2.2, 1.1, 1and 0.24 nM for native pan-BCR-ABL, mutated form, VEGFR2, FGFR1, PDGFR¦Á, mutant FLT3 phosphorylation and LYN. It potently inhibited other clinically important ABL kinase domain mutants with IC50 from 0.30 to 0.44 nM and inhibited SRC with an IC50 of 5.4 nM. It inhibits the proliferation of mutant FLT3-positive cells with an IC50 of 13 nM and that inhibits mutant FLT3 phosphorylation with an IC50 of 1 nM and the proliferation of BCR-ABL1 T315I-positive Ba/F3 cells with an IC50 of 8 nM. It inhibited all tested BCR-ABL mutants with low nM IC50s in cellular and biochemical assays, suppressed BCR-ABL(T315I)-driven tumor growth in mice, and completely abrogated resistance in cell-based mutagenesis screens. AP24534 is used for treatment of CML. It did not inhibit Aurora kinase family members, nor did it inhibit insulin receptor or cyclin- dependent kinase 2 (CDK2)/Cyclin E (IC50 > 1000-fold relative to native ABL

prudect name : AP24534 is a novel potent, orally available small molecule multitargeted kinase inhibitor with IC50 of 0.37, 2, 1.5, 2.2, 1.1, 1and 0.24 nM for native pan-BCR-ABL, mutated…

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PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 ¡À 0.112, 6.038 ¡À 0.039 and 6.009 ¡À 0.209 at pH 6.4 for the inhibition of H+, K+-ATPase activity of porcine, canine and human ion-leaky membrane vesicles, respectively. PF-03716556 is used for the treatment of gastroesophageal reflux disease. PF-03716556 is highly selective for H+, K+-ATPase in vitro. PF-03716556 displays no activity at Na+, K+-ATPase. PF-03716556 inhibits gastric acid secretion in rat and dog models. PF-03716556 has no species differences among the porcine, canine and human enzymes. PF-03716556 produced greater inhibition than revaprazan in both the in vitro (ion-tight assay) and in vivo conditions. PF-03716556 offers long-lasting and maximal efficacy within 30 min of a single dosing with responses that are maintained for at least 5 days of repeated dosing with no signs of tolerance. PF-03716556 did not exhibit any biologically relevant activity against any of the tested more than 50 (e.g., adenosine receptor) receptors, ion channels, or enzymes expressed in naïve tissues, cell lines and transfectants.

prudect name : PF-03716556 is a potent, and selective acid pump antagonist with pIC50 of 6.026 ¡À 0.112, 6.038 ¡À 0.039 and 6.009 ¡À 0.209 at pH 6.4 for the…

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In vitro, PA-824 exhibits the high activity against multidrug-resistant clinical isolates from Asia (India and South Korea) and from throughout the United States (MIC < 1 ¦Ìg/ml) and is equally active against the drug-sensitive and multidrug-resistant isolates of M. tuberculosis (MICs range, 0.039 to 0.531 ¦Ìg/ml).A recent study shows that single-nucleotide polymorphisms of PA-824 resistance genes (fgd1 [Rv0407] and ddn [Rv3547]) don¡¯t significantly affect the PA-824 MICs (¡Ü 0.25 ¦Ìg/ml).

prudect name : In vitro, PA-824 exhibits the high activity against multidrug-resistant clinical isolates from Asia (India and South Korea) and from throughout the United States (MIC < 1 ¦Ìg/ml)...

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PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 ¦ÌM and the first small molecule known to directly activate procaspase-3 to caspase-3.

prudect name : PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 ¦ÌM and the first small molecule known to directly activate procaspase-3 to caspase-3.PAC-1 Synonyms: CAS NO: 315183-21-2Molecular…

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A novel broad-spectrum HDAC(histone deacetylase) inhibitor belongs to the hydroxamate class, in Philadelphia chromosome¨Cnegative (Ph-) acute lymphoblastic leukemia (ALL). Histone deacetylases (HDACs) are responsible for deacetylating histones and nonhistone proteins, thus regulating gene transcription, protein function, and stability.Aberrant recruitment of HDACs has been shown to play an important role in leukemogenesis, and alterations in the expression and/or activity of HDACs have been also observed in solid tumors.The 50% inhibitory concentration (IC50) value for inhibition of proliferation in MOLT-4 cells is approximately 5 nM and for Reh cells is approximately 20 nM.Similar results were observed at 24 and 72 hours.

prudect name : A novel broad-spectrum HDAC(histone deacetylase) inhibitor belongs to the hydroxamate class, in Philadelphia chromosome¨Cnegative (Ph-) acute lymphoblastic leukemia (ALL). Histone deacetylases (HDACs) are responsible for deacetylating histones…

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PIK-90 is a potent and cell permeable PI3K inhibitor, with IC50 values (nM) of 11, 350, 18, and 58 for p110 ¦Á, ¦Â, ¦Ã and ¦Ä isoforms, low mTOR activity. Besides Val882 H-binding, PIK-90 uses its pyridine ring to enter the hydrophobic affinity pocket of the ATP binding site, where it also interacts with Lys833.

prudect name : PIK-90 is a potent and cell permeable PI3K inhibitor, with IC50 values (nM) of 11, 350, 18, and 58 for p110 ¦Á, ¦Â, ¦Ã and ¦Ä isoforms,…

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Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.

prudect name : Poziotinib(NOV120101; HM781-36B) is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.Poziotinib (HM781-36B) Synonyms: CAS NO: 1092364-38-9Molecular Formula: C23H21Cl2FN4O3Molecular Weight: 491.34Purity: 98% minSolubility: In…

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Indications of depression paroxetine hydrochloride, can treat obsessive compulsive disorder, panic disorder or social anxiety disorder.

prudect name : Indications of depression paroxetine hydrochloride, can treat obsessive compulsive disorder, panic disorder or social anxiety disorder.Paroxetine hydrochloride Synonyms: CAS NO: 78246-49-8Molecular Formula: C19H20FNO3.HClMolecular Weight: 365.83Purity: ≥99%Solubility: Storage:…

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