PTC124 (Ataluren) selectively induces ribosomal read-through of premature but not normal termination codons, with EC50 of 0.1 ¦ÌM, may provide treatment for genetic disorders caused by nonsense mutations (e.g. CF caused by CFTR nonsense mutation).

June 21, 2017

prudect name : PTC124 (Ataluren) selectively induces ribosomal read-through of premature but not normal termination codons, with EC50 of 0.1 ¦ÌM, may provide treatment for genetic disorders caused by nonsense…

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Dacomitinib (PF299804,PF-00299804) 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.Dacomitinib (PF299804,PF-00299804) is a quinazalone-based irreversible pan-ERBB inhibitor structurally related to CI-1033. Dacomitinib (PF299804,PF-00299804) is a potent inhibitor of EGFR-activating mutations as well as the EGFR T790M resistance mutation both in vitro and in vivo. Additionally, Dacomitinib (PF299804,PF-00299804) is a highly effective inhibitor of both the wild-type ERBB2 and the gefitinib-resistant oncogenic ERBB2 mutation identified in lung cancers. Dacomitinib (PF299804,PF-00299804) 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, Dacomitinib (PF299804,PF-00299804) also effectively inhibited wild-type ERBB2. LCK and SRC were the only other kinases inhibited by Dacomitinib (PF299804,PF-00299804) 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. Dacomitinib (PF299804,PF-00299804) is active in E-sensitive and -resistant preclinical models. Dacomitinib (PF299804,PF-00299804) had clinical activity in phase I/II trials in EGFR TK inhibitor (TKI)-refractory NSCLC.Dacomitinib (PF299804,PF-00299804) is originally developed by Seoul National University Hospital and Pfizer. The phase II clinical trials for Dacomitinib (PF299804,PF-00299804) was performing in the treatment of advanced gastric cancer.

prudect name : Dacomitinib (PF299804,PF-00299804) 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,…

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PF-04929113 (SNX-5422) is originally developed by Pfizer and Serenex, Inc., and the phase I clinical trials for PF-04929113 (SNX-5422) has been completed in the treatment of solid tumors.

prudect name : PF-04929113 (SNX-5422) is originally developed by Pfizer and Serenex, Inc., and the phase I clinical trials for PF-04929113 (SNX-5422) has been completed in the treatment of solid…

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PF-4708671 is a novel cell-permeable inhibitor of S6K1 (p70 ribosomal S6 kinase 1), with a Ki of 20 nM and IC50 of 160 nM.

prudect name : PF-4708671 is a novel cell-permeable inhibitor of S6K1 (p70 ribosomal S6 kinase 1), with a Ki of 20 nM and IC50 of 160 nM.PF-4708671;PF4708671;PF 4708671 Synonyms: CAS…

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prudect name : Prostaglandin F2aSynonyms: DinoprostCAS NO: 551-11-1Molecular Formula: C20H34O5Molecular Weight: 354.48Purity: 99%Solubility: Storage: −20°C

prudect name : Prostaglandin F2a Synonyms: DinoprostCAS NO: 551-11-1Molecular Formula: C20H34O5Molecular Weight: 354.48Purity: 99%Solubility: Storage: −20°C web site: www.medchemexpress.com

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PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha inhibitor PX-478 appears to inhibit hypoxia-inducible factor 1-alpha (HIF1A) expression, which may result in decreased expression of HIF1A downstream target genes important to tumor growth and survival, a reduction in tumor cell proliferation, and the induction of tumor cell apoptosis. The inhibitory effect of this agent is independent of the tumor suppressor genes VHL and p53 and may be related to derangements in glucose uptake and metabolism due to inhibition of glucose transporter-1 (Glut-1). PX-478 has excellent activity against established human tumor xenografts, providing tumor regressions with prolonged growth delays which correlate positively with HIF-1 levels. PX-478 is a highly water soluble molecule, with good i.v., i.p. and p.o. antitumor activity. It is rapidly absorbed following oral and i.p. administration and gives excellent Cmax and AUC via these routes.

prudect name : PX-478 is HIF-1alpha inhibitor, is also an orally active small molecule with potential antineoplastic activity. Although its mechanism of action has yet to be fully elucidated, HIF1-alpha…

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prudect name : PF-431396Synonyms: CAS NO: 717906-29-1Molecular Formula: C22H21F3N6O3SMolecular Weight: 506.50Purity: 98% minSolubility: in DMSOStorage:

prudect name : PF-431396 Synonyms: CAS NO: 717906-29-1Molecular Formula: C22H21F3N6O3SMolecular Weight: 506.50Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com

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prudect name : ParecoxibSynonyms: CAS NO: 198470-84-7Molecular Formula: C19H18N2O4SMolecular Weight: 370.42Purity: 98% minSolubility: in DMSOStorage:

prudect name : Parecoxib Synonyms: CAS NO: 198470-84-7Molecular Formula: C19H18N2O4SMolecular Weight: 370.42Purity: 98% minSolubility: in DMSOStorage: -20oC web site: www.medchemexpress.com

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prudect name : PralmorelinSynonyms: GHRP-2CAS NO: 158861-67-7Molecular Formula: C42H50N8O5Molecular Weight: 746.90Purity: 98% minSolubility: Storage: -20°C

prudect name : Pralmorelin Synonyms: GHRP-2CAS NO: 158861-67-7Molecular Formula: C42H50N8O5Molecular Weight: 746.90Purity: 98% minSolubility: Storage: -20°C web site: www.medchemexpress.com

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INCB8761(PF-4136309) is a potent, Selective, and orally bioavailable CCR2 antagonist.

prudect name : INCB8761(PF-4136309) is a potent, Selective, and orally bioavailable CCR2 antagonist.PF-4136309 Synonyms: CAS NO: 1341224-83-6Molecular Formula: C29H31F3N6O3Molecular Weight: 568.59Purity: 98% minSolubility: DMSOStorage: -20¡æ web site: www.medchemexpress.com

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