24646 Results for: "shaking+incubators"

Supplier: Aladdin Scientific

Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor ofTRK, Met (c-Met), TIE2, and VEGFR2 kinaseswith IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.TargetsMET Y1230C (Cell-free assay); TrkA (Cell-free assay); TrkC (Cell-free assay); MET Y1230C (Cell-free assay); MET D1228N (Cell-free assay) 31650,0.37 nM; 0.85 nM; 0.85 nM; 1.2 nM; 1.3 nMIn vitroAltiratinib is >10-fold selective for MET versus FMS and KIT, and >50-fold selective for MET versus ABL1, FYN, HER1 (EGFR), p38α (MAPK14), PDGFRα, PDGFRβ, RET, and SRC. Altiratinib exhibits IC50s of 0.69 nmol/L in K562 cells, 1.2 nmol/L in SK-N-SH cells for inhibition of NGF-stimulated TRKA phosphorylation.

Supplier: Aladdin Scientific

ARQ 531 ARQ 531 is an ATP-competitive tyrosine kinase inhibitor designed to target BTK with an IC50 of 0.85 nM. It also has a distinct kinase selectivity profile with strong inhibitory activity against several key oncogenic drivers from TEC, Trk and Src family kinases. TargetsBTK (Cell-free assay); BRK (Cell-dree); BRK (Cell-free assay); LCK (Cell-free); LCK (Cell-free assay) 29927,0.85 nM; 2.45 nM; 2.45 nM; 3.86 nM; 3.86 nMIn vitroARQ 531 potently inhibited BTK (IC50 = 0.85 nM), the binding potency was accompanied by long residence time (51 min). ARQ 531 selectively inhibits BCR signaling dependent PI3 K/AKT/mTOR, Ras/Raf/Erk and Rap-GTPase-Cofilin pathways in TMD8 cells. It potently inhibits proliferation of hematological malignant cell lines both sensitive and resistant to ibrutinib addicted to BCR signaling.

Supplier: REVVITY HEALTH SCIENCES, INC.

The VICTOR® Nivo™ system packs all popular detection modes into the industry’s smallest multimode reader footprint. The perfect microplate reader for everyday biochemical assays, cell-based assays, molecular biology and immunoassays. Its software interface is easy to learn and use, and lets you control the instrument from almost any device – perfect for multiuser labs. The VICTOR Nivo is a high-performance multimode microplate reader that can be equipped with all major detection technologies: Absorbance, Luminescence, Fluorescence, Time-Resolved Fluorescence, TR-FRET, Fluorescence Polarization, and Alpha Technology.

Supplier: Prosci

ANGPTL4 mainly expressed in endothelial cells (hypoxia-induced). Regulates angiogenesis and modulates tumorgenesis and directly regulates lipid, glucose, and energy metabolism. Inhibits proliferation, migration, and tubule formation of endothelial cells and reduces vascular leakage. ANGPTL4 is a protein consisting of an N-terminal coiled-coil domain and a C-terminal fibrinogen-like domain (FLD). Both domains have distinct biological functions. The coiled-coil domain is responsible for the inhibitory effects on lipoprotein lipase (LPL) converting the active form of LPL into an inactive form, and the FLD domain mediates its antiangiogenic functions. The coiled coil and the FLD domains are separated by a short linker that can be cleaved after secretion. ANGPTL4 appears on the cell surface as the full-length form, where it can be released by heparin treatment. ANGPTL4 protein is then proteolytically cleaved by proprotein convertases (PCs), including furin, PC5/6, paired basic amino acid-cleaving enzyme 4, and PC7.

Supplier: Prosci

The mucins are a family of highly glycosylated, secreted proteins with a basic structure consisting of a variable number of tandem repeats (VNTRs). Membrane-associated and secretory mucins are high molecular weight glycoproteins of the glycocalyx (polysaccharide biofilm) that protects mucosal epithelium from particulate matter and microorganisms. Epithelial mucins are large, secreted and cell surface glycoproteins crucial for adhesion modulation, signaling and epithelial cell protection. The number of repeats is highly polymorphic and varies among different alleles. The Mucin family consists of Mucins 1-4, Mucin 5 (AC and B), 6-8, 11-13 and 15-17. The Mucin 16 protein (also commonly referred to as CA125), encoded for by the gene MUC16, is a very high molecular weight tumor antigen consisting of three domains: a carboxy terminal domain, an extracellular domain and an amino terminal domain. Mucin 16, an ovarian cancer-associated antigen, is used as a marker to monitor the progress of epithelial ovarian cancer. It is a hydrophilic membrane-associated protein that may be involved in vitamin A functions.

Supplier: Prosci

This mAb recognizes Golgi complex in human cells. It is a part of a new panel of reagents, which recognizes subcellular organelles or compartments of human cells. These markers may be useful in identification of these organelles in cells, tissues, and biochemical preparations. It recognizes an antigen associated with the Golgi complex in human cells only. It can be used to stain the Golgi complex in cell or tissue preparations and can be used as a Golgi marker in subcellular fractions. It produces a diffuse staining pattern of the Golgi zone in normal and malignant cells and may be used to stain Golgi complex of cells in frozen tissue sections. It can also be used with paraformaldehyde fixed frozen tissue or cell preparations. This mAb is an excellent marker for human cells in xenographic model research. It reacts specifically with human cells.

Supplier: Prosci

ANGPTL4 mainly expressed in endothelial cells (hypoxia-induced). Regulates angiogenesis and modulates tumorgenesis and directly regulates lipid, glucose, and energy metabolism. Inhibits proliferation, migration, and tubule formation of endothelial cells and reduces vascular leakage. ANGPTL4 is a protein consisting of an N-terminal coiled-coil domain and a C-terminal fibrinogen-like domain (FLD). Both domains have distinct biological functions. The coiled-coil domain is responsible for the inhibitory effects on lipoprotein lipase (LPL) converting the active form of LPL into an inactive form, and the FLD domain mediates its antiangiogenic functions. The coiled coil and the FLD domains are separated by a short linker that can be cleaved after secretion. ANGPTL4 appears on the cell surface as the full-length form, where it can be released by heparin treatment. ANGPTL4 protein is then proteolytically cleaved by proprotein convertases (PCs), including furin, PC5/6, paired basic amino acid-cleaving enzyme 4, and PC7.

Supplier: Aladdin Scientific

CCT245737 (SRA737, PNT-737) is an orally activeCHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. TargetsChk1 (Cell-free assay) 1.4 nMIn vitroCCT245737 is a potent inhibitor of recombinant human CHK1 with IC50 of 1.4±0.3 nM (mean±SD, n = 3, EZ Reader II assay). There is > 1,000-fold selectivity for CHK1 versus the functionally important kinases CDK1 and CHK2 (IC50=1.26 to 2.44 and 9.03 μM, respectively), and at least a 90-fold selectivity against cross-reacting kinases such as ERK8, PKD1, RSK1 and 2. CCT245737 potently inhibits cellular CHK1 activity (IC50 30 to 220 nM) and enhances gemcitabine and SN38 cytotoxicity in multiple human tumor cell lines and human tumor xenograft models. It can abrogate an etoposide-induced G2/M arrest. CCT245737 has high cell permeability, as measured by transport across a CaCo2 cell monolayer.

Supplier: IBI Scientific

I-Blue Midi Plasmid Endotoxin-Free Kits optimize isolation of plasmid DNA from E.coli with a simple lysis, bind, wash, and elute protocol. The kits include I-Blue lysis buffer, which helps prevent common handling errors, ensuring efficient cell lysis and SDS precipitation.

Supplier: Prosci

Estrogen receptors (ER) are members of the steroid/thyroid hormone receptor superfamily of ligand-activated transcription factors. Estrogen receptors, including alpha and beta, contain DNA binding and ligand binding domains and are critically involved in regulating the normal function of reproductive tissues. They are located in the nucleus, though some estrogen receptors associate with the cell surface membrane and can be rapidly activated by exposure of cells to estrogen. ER alpha and beta are differentially activated by various ligands. Ligand interaction triggers a cascade of events, including dissociation from heat shock proteins, recepter dimerization, phosphorylation and the association of the hormone activated receptor with specific regulatory elements in target genes. Evidence suggests that ER alpha and beta may be regulated by distinct mechanisms even though they share many functional characteristics.

Supplier: Prosci

This monoclonal antibody is part of a new panel of reagents, which recognizes subcellular organelles or compartments of human cells. These markers may be useful in identification of these organelles in cells, tissues, and biochemical preparations. This mAb recognizes the double stranded DNA in human cells. It can be used to stain the nuclei in cell or tissue preparations and can be used as a nuclear marker in human cells. This mAb produces a homogeneous staining pattern in the nucleus of normal and malignant cells.,Double Stranded deoxyribonucleic acid (ds DNA) is the genetic material of all cells and many viruses and is a polymer of nucleotides. The monomer consists of phosphorylated 2-deoxyribose N-glycosidically linked to one of four bases, adenine, cytosine, guanine or thymine. These are linked together by 3',5'-phosphodiester bridges. In the Watson-Crick double-helix model, two complementary strands are wound in a right-handed helix and held together by hydrogen bonds between complementary base pairs.

Supplier: Aladdin Scientific

CBL0137 HCl CBL0137 (CBLC137, Curaxin 137) HCl activates p53 and inhibits NF-kB with EC50 s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex). TargetsFACT ; p53 (Cell-free assay); NF-κB (Cell-free assay) ; 0.37 μM(EC50); 0.47 μM(EC50)In vitroCBL0137 is a potent inducer of apoptosis in pancreatic cancer cell lines and is toxic not only for proliferating bulk tumor cells, but also for pancreatic cancer stem cells. CBL0137 and related molecules can simultaneously activate p53 and inhibit cellular stress pathways mediated by NF-κB and HSF-1. CBL0137 binds DNA but does not cause any sort of chemical modifications in DNA and therefore lacks genotoxicity. However, CBL0137 binding to DNA leads to functional inactivation of the Facilitates Chromatin Transcription (FACT) complex, a chromatin remodeling complex involved in transcription, replication, and DNA repair. In CBL0137-treated cells, FACT is lost from the nucleoplasm and trapped in chromatin, resulting in the inhibition of FACT-dependent transcription, including NF-kB-mediated transcription.

Supplier: Lonza

The ToxiLight® Bioassay kit is a bioluminescent, non-destructive cytolysis assay kit designed to measure the release of the enzyme, adenylate kinase (AK), from damaged cells. AK is a robust protein present in all eukaryotic cells, which is released into the culture medium when cells die.

Supplier: Aladdin Scientific

ARS-853 (ARS853) ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis .Targets K-Ras(G12C) (in H358 cells) 2.5 μM In vitro ARS-853 treatment of KRASG12C cells led to a dose-dependent and nearly complete inhibition of CRAF-RBD (RBD)-mediated pulldown of KRAS from lysates, with an IC50 of approximately 1 μmol/L. Treatment of H358 cells by ARS-853 resulted in a significant loss of KRAS–CRAF interactions. Consistent with an inactive state of KRASG12C once bound to ARS-853, downstream signaling through both MAPK (including pMEK, pERK, and pRSK) and PI3K signaling (pAKT) pathways was inhibited by ARS-853 in H358 and other KRASG12C cell lines. The inhibition of RAF-RBD pulldown and KRAS downstream signaling was sustained over a period of 72 hours, accompanied by G1 cell-cycle arrest, loss of Cyclin D1 and Rb expression, and an increase in the cell-cycle inhibitor p27 KIP1.

Supplier: Sedia Biosciences

Sedia’s Asanté™ Dried Blood Specimen Collection Strips (Asanté™ Strips) are intended for the collection, transport, storage, testing, and archiving of blood specimens, including finger-stick blood, venous blood, serum, or plasma.

Supplier: Genetex

Water is a critical component of all living cells. Interestingly, tissue membranes show a great degree of water permeability. Mammalian red cells, renal proximal tubules, and descending thin limb of Henle are extraordinarily permeable to water. Water crosses hydrophobic plasma membranes either by simple diffusion or through a facilitative transport mechanism mediated by special protein ""aquaporin"". Over the last decade, genes for several members of aquaporin family have been cloned, expressed, and their distribution studied in many tissues. AQP0 or MIP26 (major intrinsic protein 26kD), and Aquaporin-1 (AQP1, purified from red cells) also called CHIP-28 (channel forming integral protein, 28kD; 268aa; gene locus 7p14) has been the foundation of the growing family of aquaporin. The lens specific AQP0 represents up to 80% of total lens membrane protein. Defects in MIP26 are cause of autosomal dominant cataract. The cataract Fraser mutation (CAT-FR or Shriveled) is a transposon-induced splicing error that substitutes a long terminal repeat sequence for the c-terminus of MIP. The lens opacity mutation (LOP) is an amino acid substitution that inhibits targeting of MIP to the cell membrane.

Supplier: Rockland Immunochemical

IL-1 beta (also known as Interleukin-1 beta, IL-1ß and catabolin) is produced by activated macrophages. IL-1 stimulates thymocyte proliferation by inducing IL-2 release, B-cell maturation and proliferation, and fibroblast growth factor activity. IL-1 proteins are involved in the inflammatory response, being identified as endogenous pyrogens, and are reported to stimulate the release of prostaglandin and collagenase from synovial cells. IL-1ß is a monomeric secreted protein that may be released by damaged cells or is secreted by a mechanism differing from that used for other secretory proteins. Anti-IL-1 beta antibody is ideal for investigators involved in Cardiovascular and Immunology research.

Supplier: Aladdin Scientific

BS-181 HCl is a highly selectiveCDK7 inhibitor withIC50 of 21 nM. It is more than 40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9. TargetsCDK7 (Cell-free assay) 21 nMIn vitroBS-181 is a small molecule inhibitor of CDK7 in a cell-free environment, which displays more potential activity than roscovitine with IC 50 of 510 nM. Among the CDKs and other 69 kinases from many different classes, BS-181 shows high inhibitory selectivity for CDK7, inhibits CDK2 at concentrations lower than 1 μM which being inhibited 35-fold less potently (IC50 with 880 nM) than CDK7, shows slight inhibition for CDK1, CDK4, CDK5, CDK6 and CDK9 with IC50 values higher than 3.0 μM, and only shows inhibition for several kinases from other classes at high concentrations (>10 μM). BS-181 promotes cell cycle arrest and inhibits the cancer cell growth of a range of tumor types, including breast, lung, prostate and colorectal cancer with IC50 in the range of 11.5 to 37 μM.

Supplier: MICROBIOLOGICS, INC.

EZ-Accu Shot™ Select boasts all the same features and benefits as the original EZ-Accu Shot™, but includes six compendial QC microorganism strains for Growth Promotion Testing in one convenient package. EZ-Accu Shot™ Select lyophilized QC microorganism preparations are designed to deliver 10-100 CFU per 0.1 mL of hydrated suspension as recommended by the USP/JP/Ph. Eur. With little to no preparation time required and up to eight hours of stability, EZ-Accu Shot™ Select adds efficiency and flexibility to QC laboratories’ busy schedules. Each 1.2 mL vial of hydrated suspension offers 10 inocula. For added convenience, individual peel-off informational labels are included for each strain.

Supplier: Prosci

VASP (vasodilator-stimulated phosphoprotein) is a proline-rich protein substrate of cAMP- and cGMP-dependent protein kinases. VASP is an actin-associated protein involved in a range of processes dependent on cytoskeleton remodeling and cell polarity such as axon guidance, lamellipodial and filopodial dynamics, platelet activation and cell migration. VASP promotes actin filament elongation. It protects the barbed end of growing actin filaments against capping and increases the rate of actin polymerization in the presence of capping proteins. VASP stimulates actin filament elongation by promoting the transfer of profilin-bound actin monomers onto the barbed end of growing actin filaments and it plays a role in actin-based mobility of Listeria monocytogenes in host cells. It regulates actin dynamics in platelets and plays an important role in regulating platelet aggregation. VASP phosphorylation is used to monitor the effect of so-called antiplatelet drugs that reduce platelet reactivity and are used to prevent stent thrombosis, strokes and heart attacks in patients. Phosphorylation of VASP at Ser157 causes a mobility shift in SDS gel electrophoresis from 46 to 50kDa, which has been used as a convenient marker to monitor cyclic nucleotide-dependent protein kinase activity.

Supplier: Omega Bio-Tek

The E.Z.N.A.® FFPE DNA Kit is designed for fast and easy purification of DNA from formalin-fixed, paraffin-embedded (FFPE) tissue sections

Supplier: MilliporeSigma

Pellet Paint® Co-Precipitant is a visible dye-labeled carrier formulated specifically for use in alcohol precipitation of nucleic acids.

Supplier: Bulldog Bio

PNGase F PRIME is a mutant recombinant PNGase F cloned from Flavobacterium meningosepticum and expressed and purified from E. coli. The proprietary changes made to PNGase F have been shown to have unique characteristics when compared to other commercially-available sources of PNGase F. Data generated by independent labs shows that PRIME works on native glycoproteins and serum glycoproteins in minutes at room temperature. Glycan analysis of the digestion products shows that PNGase F PRIME digestion led to more complete glycan release and also allowed for the cleavage of glycans not released by the commercially-available enzymes when used at the same concentrations with the same digestion conditions. This advancement benefits applications that seek to understand glycobiology in a natural milieu. Preliminary data indicates that PNGase F PRIME has a higher specificity towards complex (tri and tetra-antennary) sialylated structures compared to the commercially sourced enzyme. Additionally, the work presented in this Analytical Chemistry paper utilized PNGase F PRIME for all in situ tissue work as the commercially-available PNGase enzymes did not work on native tissue to allow glycan recognition.

Supplier: Aladdin Scientific

Brilanestrant (GDC-0810, ARN-810) is a potentER-αbinder (ER-α, IC50 = 6.1 nM; ER-β, IC50 = 8.8 nM), a full transcriptional antagonist with no agonism and displays good potency and efficacy in ER-α degradation (EC50 = 0.7 nM) and MCF-7 breast cancer cell viability (IC50 = 2.5 nM) assays with good selectivity over other nuclear hormone receptors. TargetsERα (Cell-free); ERβ (Cell-free) 6.1 nM; 8.8 nM In vitro In cell-free radio-ligand competitive binding assays, GDC-0810 binds both ERα and ERβ with low nanomolar affinity. GDC-0810 has little to no inhibition against CYP1A2, CYP2D6, or CYP3A4 (IC50 > 20 μM), modest inhibitory effect on CYP2C9 and CYP2C19 (IC50 = 2.2 and 3.3 μM respectively), and potent inhibition of CYP2C8 (IC50 of <0.1 μM). Selectivity of GDC-0810 over other nuclear hormone receptors is also found to be good. In transcriptional reporter assays for the mineralocorticoid (MR), progesterone-A (PR-A), progesterone (PR-B), and glucocorticoid (GR) receptors, GDC-0810 has minimal activity (IC50 > 1 μM).

Supplier: Alkali Scientific

Effortlessly extract and amplify DNA from tissue samples with the Radiant™ DNA extract and amplify tissue PCR kit.

Supplier: Bulldog Bio

PNGase F PRIME is a mutant recombinant PNGase F cloned from Flavobacterium meningosepticum and expressed and purified from E. coli. The proprietary changes made to PNGase F have been shown to have unique characteristics when compared to other commercially-available sources of PNGase F. Data generated by independent labs shows that PRIME works on native glycoproteins and serum glycoproteins in minutes at room temperature. Glycan analysis of the digestion products shows that PNGase F PRIME digestion led to more complete glycan release and also allowed for the cleavage of glycans not released by the commercially-available enzymes when used at the same concentrations with the same digestion conditions. This advancement benefits applications that seek to understand glycobiology in a natural milieu. Preliminary data indicates that PNGase F PRIME has a higher specificity towards complex (tri and tetra-antennary) sialylated structures compared to the commercially sourced enzyme. Additionally, the work presented in this Analytical Chemistry paper utilized PNGase F PRIME for all in situ tissue work as the commercially-available PNGase enzymes did not work on native tissue to allow glycan recognition.

Supplier: Prosci

Profilin (PFN1) is a ubiquitous small (12-15kDa) phosphoinositide and poly-L-proline binding protein that plays a role in signal transduction pathways and actin filament dynamics. There are two mammalian profilins with similar biochemical properties. Whereas profilin I appears to be highly expressed in most tissues except for skeletal muscle, profilin II is predominantly expressed in brain and at lower levels also in skeletal muscle, uterus and kidney. Profilin is a mainly cytosolic protein with higher concentrations in dynamic membrane areas like the leading edge and ruffling membranes. Profilin binding to PIP2 interferes with PIP2 hydrolysis by soluble phospholipase C-gamma, an inhibition that can be overcome by tyrosine phosphorylation of PLC-gamma. Besides actin monomer sequestration and stimulation of actin nucleotide exchange, profilin can also promote cellular actin filament growth. Profilin is involved in the actin dependent intracellular motility of cytopathogenic bacteria, the regulation of cell adhesion and possibly also in linking the actin cytoskeleton and endocytosis. Profilin has been found to associate with defined complexes containing proteins such as Arp2/3 or the Rho/Rac pathways constituents ROCK-II and HEM2/NAP1. Defects in PFN1 are the cause of amyotrophic lateral sclerosis 18 (ALS18).

Supplier: Prosci

Processes such as transcription, repair and replication that require efficient DNA recognition are dependent on modulation of chromatin structure. Chromatin relaxation is a critical event that occurs during DNA repair and is associated with the negatively charged polymer of adenosine 5'-diphosphate (ADP)-ribose (PAR). PAR is synthesized from nicotinamide adenine dinucleotide (NAD+) by the poly(ADP-ribose) polymerase protein family (PARPs), of which PARP-1 (and to a lesser extent PARP-2) respond to DNA-strand breaks. PARP-1 is selectively activated by DNA strand breaks to catalyze the addition of long branched chains of PAR to a variety of nuclear proteins, most notably PARP itself. The amount of PAR formed in living cells with DNA damage is commensurate with the extent of the damage. Under DNA damage conditions, PAR undergoes a rapid turnover, with a half-life in the range of minutes, as PAR is rapidly hydrolyzed and converted to free ADP-ribose by the enzyme poly(ADP-ribose)glycohydrolase (PARG). PAR regulates not only cell survival and cell-death programmes, but also an increasing number of other biological functions with which novel members of the PARP family have been associated. These include transcriptional regulation, cell division, intracellular trafficking, inflammation and energy metabolism.

Supplier: Biosensis

Tyrosine hydroxylase is an excellent marker for dopaminergic and noradrenergic neurons. Tyrosine hydroxylase (a.k.a. tyrosine 3-monooxygenase) is the enzyme responsible for catalyzing the conversion of the amino acid L-tyrosine to L-3,4-dihydroxyphenylalanine (L-DOPA). L-DOPA is a precursor for dopamine, which, in turn, is a precursor for the important neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline). Tyrosine hydroxylase catalyzes the rate limiting step in this synthesis of catecholamines. In humans, tyrosine hydroxylase is encoded by the TH gene, and the enzyme is present in the central nervous system (CNS), peripheral symphatic neurons and the adrenal medulla. The enzymatic activity of TH requires ferrous ions as cofactors and is believed to be regulated by phosphorylation. At least four isoforms of human TH have been identified which result from alternative splicing. Tyrosine hydroxylase, phenylalanine hydroxylase and tryptophan hydroxylase together make up the family of aromatic amino acid hydroxylases (AAAHs). http://en.wikipedia.org/wiki/Tyrosine_hydroxylase

Supplier: Aladdin Scientific

Bimiralisib (PQR309) is a novel brain-penetrant dualPI3 K/mTORinhibitor within vitro and in vivo antilymphoma activity. It displays excellent selectivity versus PI3 K-related lipid kinases, protein kinases and unrelated targets. TargetsPI3 Kα (Cell-free assay); PI3 Kβ (Cell-free assay); mTOR (Cell-free assay); PI3 Kγ (Cell-free assay); PI3 Kδ (Cell-free assay) 1.5 nM(Kd); 11 nM(Kd); 12 nM(Kd); 25 nM(Kd); 25 nM(Kd)in vitro PQR309 showsin vitro activity with a median IC50 value of 233 nmol/L (95% CI, 174 to 324 nmol/L) in most of the tesed lymphoma cell lines (increasing doses, 72 hours). The arrest in proliferation is mainly due to cell cycle arrest with a block in G1 rather than to apoptosis, limited to only 2/7 cell lines. PQR309 is more active in B-cell lymphoma cell lines (DLBCL, MCL, CLL, and SMZL) than in the T-cell derived ALCL. PQR309 inhibits PI3 K/mTOR signaling in lymphoma cell lines. It hasin vitro and in vivo antilymphoma activity as single agent and in combination.\xa0 in vivo PQR309 is orally available, crosses the blood−brain barrier, and displayed favorable pharmacokinetic parameters in mice, rats, and dogs.