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PF299804 is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.PF299804 is a quinazalone-based irreversible pan-ERBB inhibitor structurally related to CI-1033. PF299804 is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, PF299804 is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. PF299804 effectively inhibited the in vitro kinase activity of wild-type EGFR with similar efficacy as gefitinib, erlotinib, andCI-1033. In contrast to gefitinib and erlotinib, PF299804 also effectively inhibited wild-type ERBB2. LCK and SRC were the only other kinases inhibited by PF299804 although with >10 fold higher IC50 than against EGFR. PF299804 inhibited cellular EGFR and ERBB 2 with IC50 of 5.8 and 41 nM in NIH3T3/EGFR cell and NIH3T3/ERBB2 cell, respectively. PF299804 is active in E-sensitive and -resistant preclinical models. PF299804 had clinical activity in phase I/II trials in EGFR TK inhibitor (TKI)-refractory NSCLC. PF299804 is originally developed by Seoul National University Hospital and Pfizer. The phase II clinical trials for PF299804 was performing in the treatment of advanced gastric cancer.

June 21, 2017

prudect name : PF299804 is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2…

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PF-04691502 is a potent and selective dual PI3K/mTOR inhibitor to phosphorylation of AKT T308 and AKT S473 with IC50 of 7.5 and 3.8 nM, respectively. PF-04691502 is an ATP-competitive inhibitor which potently inhibits recombinant class I PI3K and mTOR in biochemical assays and suppresses transformation of avian fibroblasts mediated by wild type PI3K¦Ã, ¦Äor mutant PI3K¦Á.PF-04691502 has potential antineoplastic activity. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF-04691502 decreases phosphorylation of AKT T308 and AKT S473 with IC50 ranging from 7.5 to 47 nM and from 3.8 to 20 nM respectively, and inhibits cell proliferation with IC50 ranging from 179 to 313 nM. In addition, PF-04691502 inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. PF-04691502 inhibits mTORC1 activity in cells as measured by PI3K-independent nutrient stimulated assay, with an IC50 of 32 nM and inhibits the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1 and S6RP. Short-term exposure to PF-04691502 predominantly inhibits PI3K, while mTOR inhibition persists for 24-48 hours. PF-04691502 causes cell cycle G1 arrest, concomitant with upregulation of p27 Kip1 and reduction of Rb. Antitumor activity is observed in U87 (PTEN null), SKOV3 (PIK3CA mutation) and gefitinib- and erlotinib-resistant NSCLC xenografts. PF-04691502 is originally developed by Pfizer. PF-04691502 is under a phase II clinical trial in the treatment of endometrial neoplasms

prudect name : PF-04691502 is a potent and selective dual PI3K/mTOR inhibitor to phosphorylation of AKT T308 and AKT S473 with IC50 of 7.5 and 3.8 nM, respectively. PF-04691502 is…

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PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.

prudect name : PF-04449913 is a potent and orally bioavailable inhibitor of smoothened with IC50 of 5 nM(Gli-luciferase reporter reporter in C3H10T1/2); the hedgehog pathway inhibitor.PF 04449913 Synonyms: CAS NO:…

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PP1 is a potent and selective Src family protein tyrosine kinase inhibitor. PP1 effectively blocks TGF-beta1-induced cell migration and invasion in both established and primary carcinoma cells. PP1 blocks TGF-beta1-mediated cellular responses by direct and differential inhibition of type I and type II TGF-beta receptors. PP1 was also found to potentiate tumor-suppressive effect of connexin 32 gene in renal cancer cells.

prudect name : PP1 is a potent and selective Src family protein tyrosine kinase inhibitor. PP1 effectively blocks TGF-beta1-induced cell migration and invasion in both established and primary carcinoma cells….

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Pixantrone is a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA replication and tumor cell cytotoxicity. Pixantrone is a potentially more effective, less cardiotoxic alternative to doxorubicin for patients with aggressive non-Hodgkin lymphoma (aNHL).

prudect name : Pixantrone is a synthetic, noncardiotoxic aza-anthracenedione analogue with potential antineoplastic activity. Pixantrone intercalates into DNA and induces topoisomerase II-mediated DNA strand crosslinks, resulting in inhibition of DNA…

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pirarubicin is an analogue of the anthracycline antineoplastic antibiotic doxorubicin. Pirarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. This agent is less cardiotoxic than doxorubicin and exhibits activity against some doxorubicin-resistant cell lines.

prudect name : pirarubicin is an analogue of the anthracycline antineoplastic antibiotic doxorubicin. Pirarubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA…

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PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).

prudect name : PD 169316 is a potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).PD 169316 Synonyms: CAS NO: 152121-53-4Molecular Formula: C20H13FN4O2Molecular Weight: 360.34Purity: 98% minSolubility:…

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Prucalopride short-term treatment of severe chronic constipation can significantly improve bowel function, reduce symptoms of constipation.

prudect name : Prucalopride short-term treatment of severe chronic constipation can significantly improve bowel function, reduce symptoms of constipation.Prucalopride Succinate Synonyms: CAS NO: 179474-85-2Molecular Formula: C18H26ClN3O3.C4H6O4Molecular Weight: 485.96Purity: 99%Solubility: In…

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Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin D1 and cdk5-p35 respectively.

prudect name : Purvalanol B(NG-95) is a cyclin-dependent kinase inhibitor with IC50 values of 6, 6, 9, > 10,000, and 6 nM for cdc2/cyclin B, cdk2/cyclin A, cdk2/cyclin E, cdk4/cyclin…

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Plerixafor inhibits CXCL12-mediated chemotaxis with a potency slightly better than its affinity for CXCR4.Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits SDF-1 mediated GTP-binding, SDF-1 mediated calcium flux and SDF-1 stimulated chemotaxis with IC50 of 27 nM, 572 nM and 51 nM, respectively. Plerixafor does not inhibit calcium flux against cells expressing CXCR3, CCR1, CCR2b, CCR4, CCR5 or CCR7 when stimulated with their cognate ligands, Nor does Plerixafor inhibit receptor binding of LTB4. Plerixafor does not, on its own, induce a calcium flux in the CCRF¨CCEM cells, which express multiple GPCRs including CXCR4, CCR4 and CCR7.

prudect name : Plerixafor inhibits CXCL12-mediated chemotaxis with a potency slightly better than its affinity for CXCR4.Plerixafor also antagonizes SDF-1/CXCL12 ligand binding with an IC50 of 651 nM. Plerixafor inhibits…

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