Palomid 529 (P529) is a novel potent antitumour PI3K/Akt/mTOR inhibitor with a GI50 of <35 ¦ÌM in the NCI-60 cell lines panel. Palomid 529 (P529) inhibits the TORC1 and TORC2 complexes and shows both inhibition of Akt signaling and mTOR signaling similarly in tumor and vasculature. Palomid 529 (P529) inhibits tumor growth, angiogenesis, and vascular permeability. However, Palomid 529 (P529) has the additional benefit of blocking pAktS473 signaling consistent with blocking TORC2 in all cells and thus bypassing feedback loops that lead to increased Akt signaling in some tumor cells. Palomid 529 (P529) inhibited both VEGF-driven (IC50 = 20 nM) and bFGF-driven (IC50 = 30 nM) endothelial cell proliferation and retained the ability to induce endothelial cell apoptosis. In addition, Palomid 529 (P529) significantly enhanced the antiproliferative effect of radiation in prostate cancer cells (PC-3).

 June 21, 2017

prudect name : Palomid 529 (P529) is a novel potent antitumour PI3K/Akt/mTOR inhibitor with a GI50 of

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VEGFR enzyme assays for VEGGR1,VEGFR2, and VEGFR3 were running in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein encoding the catalytic c-terminus of human VEGFR receptor kinases 1, 2, or 3. Pazopanib HCl showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively. Significant activity was also seen against the closely related tyrosine receptor kinases PDGFR beta, c-Kit, FGF-R1, and c-fms with IC50¡¯s of 84, 74, 140,and 146 nM, respectively. In cellular assays, in addition to inhibiting the VEGF-induced proliferation of HUVECs, Pazopanib HCl potently inhibited VEGF-induced phosphorylation of VEGFR-2 in HUVEC cells with an IC50 of ∼8 nM. The cytochrome P450 profile was also improved with inhibition >10 ¦ÌM against the isozymes tested, with the exception of 2C9 (7.9 ¦ÌM).

prudect name : VEGFR enzyme assays for VEGGR1,VEGFR2, and VEGFR3 were running in homogeneous time-resolved fluorescence (HTRF) format in 384-well microtiter plates using a purified, baculovirus-expressed glutathione-S-transferase (GST) fusion protein…

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BAY 57-1293 represents a new class of potent inhibitors of herpes simplex virus (HSV) that target the virus helicase primase complex.

prudect name : BAY 57-1293 represents a new class of potent inhibitors of herpes simplex virus (HSV) that target the virus helicase primase complex.Pritelivir (BAY 57-1293) Synonyms: CAS NO: 348086-71-5Molecular…

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PP-121 selectivity interacts within a hydrophobic pocket that is conserved between both tyrosine kinases and PI3Ks, not serine-threonine kinases. PP-121 makes a hydrogen bond to Glu310 in Src, effectively substituting for the structural role of the catalytic lysine and resulting in the ordering of helix C and stabilization of an active conformation. PP-121 also inhibits other PI3Ks including p110¦Á and DNA-PK with IC50 of 52 nM and 60 nM, respectively. PP-121 potently and dose-dependently blocks the phosphorylation of Akt, p70S6K and S6 in two glioblastoma cell lines, U87 and LN229. PP-121 potently inhibits the proliferation of a subset of the tumor cell lines by direct inhibition of PI3Ks and mTOR. PP-121 induces a G0/G1 arrest in LN220, U87 and Seg1 cells. PP-121 also blocks tyrosine phosphorylation induced by v-Src in NIH3T3 cells transformed with v-Src(Thr338). PP-121 could restore actin stress fiber staining in NIH3T3 cells transformed with v-Src(Thr338). PP-121 at a low concentration of 40 nM inhibits Ret autophosphorylation in TT thyroid carcinoma cells that express the C634W oncogenic Ret mutant35. PP-121 inhibits cell proliferation with IC50 of 50 nM in TT thyroid carcinoma cells. PP-121 inhibits cell proliferating stimulated only with VEGF with IC50 of 41 nM in human umbilical vein endothelial cells (HUVECs). PP-121 directly inhibits Bcr-Abl induced tyrosine phosphorylation, resulting in drug-induced apoptosis in K562 cells and a combination of apoptosis and cell cycle arrest in Bcr-Abl expressing BaF3 cells.

prudect name : PP-121 selectivity interacts within a hydrophobic pocket that is conserved between both tyrosine kinases and PI3Ks, not serine-threonine kinases. PP-121 makes a hydrogen bond to Glu310 in…

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PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and <0.1 ¦ÌM for PI3K-¦Á and mTOR, respectively. Intravenous administration of PKI-587 exhibits excellent antitumor activity in vitro and in vivo in both subcutaneous and orthotopic xenograft tumor models. Phosphorylation of PI3K/mTOR effectors (e.g., Akt) effectively inhibited by PKI-587. And PKI-587 induced apoptosis in human tumor cell lines with elevated PI3K/mTOR signaling. In vivo, PKI-587suppressed tumor growth in breast (MDA-MB-361, BT474), colon (HCT116), lung (H1975), and glioma (U87MG) xenograft models. PKI-587 (25 mg/kg, single dose i.v.) suppressed Akt phosphorylation [at threonine(T)308 and serine(S)473] for up to 36 hours, with cleaved PARP (cPARP) evident up to 18 hours in MDA-MB-361 tumors. PKI-587 also caused regression in other tumor models, and efficacy was enhanced when given in combination with PD0325901 (MEK 1/2 inhibitor), irinotecan (topoisomerase I inhibitor), or HKI-272 (neratinib, HER2 inhibitor).

prudect name : PKI-587 is a highly potent dual PI3K/mTOR kinase inhibitor with IC50 of 0.4 nM and

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Pexidartinib(PLX-3397) is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.

prudect name : Pexidartinib(PLX-3397) is a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.Pexidartinib(PLX-3397) Synonyms: CAS NO: 1029044-16-3Molecular Formula: C20H15ClF3N5Molecular Weight: 417.81Purity: 98%…

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Biological Activity of Perifosine: A p.o.-bioavailable ALK(Alkylphospholipids),inhibits Akt activation. Targeting cellular membranes, perifosine modulates membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. Perifosine has a lower gastrointestinal toxicity profile than the related agent miltefosine. Immortalized keratinocytes (HaCaT) as well as head and neck squamous carcinoma cells were sensitive to the antiproliferative properties of perifosine with an IC50 of 0.6¨C8.9 ¦ÌM

prudect name : Biological Activity of Perifosine: A p.o.-bioavailable ALK(Alkylphospholipids),inhibits Akt activation. Targeting cellular membranes, perifosine modulates membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in…

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PF-00562271 is a potent ATP-competitive FAK and proline-rich tyrosine kinase (Pyk2) inhibitor with potential antineoplastic and antiangiogenic activities. Focal adhesion kinase (FAK) transduces signaling from integrins and growth factors to modulate tumor cell invasion, proliferation and survival. Focal adhesion kinase (FAK) is a non-receptor protein tyrosine kinase located in the cytoplasm at focal adhesions ¨C sites that link the extracellular matrix to the cytoplasmic cytoskeleton. Not only do FAKs therefore play a pivotal role in cell migration, but they also influence cell survival and are upregulated in a broad spectrum of epithelial cancers. PF-00562271 may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by PF-00562271 may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.

prudect name : PF-00562271 is a potent ATP-competitive FAK and proline-rich tyrosine kinase (Pyk2) inhibitor with potential antineoplastic and antiangiogenic activities. Focal adhesion kinase (FAK) transduces signaling from integrins and…

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PD 0332991 is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. This compound is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4) (IC50, 0.011 ¦Ìmol/L) and Cdk6 (IC50, 0.016 ¦Ìmol/L), having no activity against a panel of 36 additional protein kinases. Therapeutic doses of PD0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and downregulation of genes under the transcriptional control of E2F.

prudect name : PD 0332991 is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. This compound is a highly specific inhibitor of cyclindependent kinase 4 (Cdk4)…

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prudect name : Pneumocandin B0Synonyms: CAS NO: 135575-42-7Molecular Formula: C50H80N8O17Molecular Weight: 1065.21Purity: 98% minSolubility: Storage:

prudect name : Pneumocandin B0 Synonyms: CAS NO: 135575-42-7Molecular Formula: C50H80N8O17Molecular Weight: 1065.21Purity: 98% minSolubility: Storage: −20°C web site: www.medchemexpress.com

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