Andreas Zoephel
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View article: Supplementary Figure S2: Western blot analysis of MAPK pathway inhibition by BI 847325 in BRAF-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S2: Western blot analysis of MAPK pathway inhibition by BI 847325 in BRAF-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
(A), MEK1 and phospho-MEK1/2; (B) ERK1/2 and phospho-ERK1/2.
View article: CD-20-0142R1_Supplementary_Figures_S1-S5.docx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Figures_S1-S5.docx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Supplementary Figures S1-S5
View article: Supplementary Materials and Methods, Tables S1 through S3 and Figures S1 and S2 from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis
Supplementary Materials and Methods, Tables S1 through S3 and Figures S1 and S2 from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis Open
Supplementary Materials and Methods, Tables S1 through S3 and Figures S1 and S2 - Supplementary Materials and Methods: The sources, application and dilution of the antibodies used for Western blotting (WB) and immunohistochemical (IHC) ana…
View article: Supplementary Table S1, S2, S3, S4 and Supplementary Figure legends from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Table S1, S2, S3, S4 and Supplementary Figure legends from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
Supplementary Table S1: Statistics of data collection and processing of AuroraB/INCENP in complex with BI 847325; Supplementary Table S2: Statistics of data collection and processing of MEK1 in complex with BI 847325; Supplementary Table S…
View article: Supplementary Figure S1: Chemical structure of the AK-B inhibitor BI 811283. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S1: Chemical structure of the AK-B inhibitor BI 811283. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
Chemical structure of BI 811283: 2,3-diamino-pyrimidine
View article: Supplementary Materials and Methods, Tables S1 through S3 and Figures S1 and S2 from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis
Supplementary Materials and Methods, Tables S1 through S3 and Figures S1 and S2 from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis Open
Supplementary Materials and Methods, Tables S1 through S3 and Figures S1 and S2 - Supplementary Materials and Methods: The sources, application and dilution of the antibodies used for Western blotting (WB) and immunohistochemical (IHC) ana…
View article: Supplementary Figure S5: Efficacy of BI 847325 in the MIAPaCa-2 (KRASG12C) model of human pancreatic adenocarcinoma. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S5: Efficacy of BI 847325 in the MIAPaCa-2 (KRASG12C) model of human pancreatic adenocarcinoma. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
BomTac:NMRI-Foxn1nu mice bearing human MIAPaCa-2 tumors were treated with vehicle, BI 847325 at 10 mg/kg daily p.o., AZD6244 at 25 mg/kg twice daily p.o., GSK 1120212 at 0.25 mg/kg twice daily p.o. Data is plotted as average tumor volume w…
View article: Data from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis
Data from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis Open
Inhibition of the IGF1R, INSRA, and INSRB receptor tyrosine kinases represents an attractive approach of pharmacologic intervention in cancer, owing to the roles of the IGF1R and INSRA in promoting cell proliferation and survival. However,…
View article: Data from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Data from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
Although the MAPK pathway is frequently deregulated in cancer, inhibitors targeting RAF or MEK have so far shown clinical activity only in BRAF- and NRAS-mutant melanoma. Improvements in efficacy may be possible by combining inhibition of …
View article: Data from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis
Data from BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis Open
Inhibition of the IGF1R, INSRA, and INSRB receptor tyrosine kinases represents an attractive approach of pharmacologic intervention in cancer, owing to the roles of the IGF1R and INSRA in promoting cell proliferation and survival. However,…
View article: Supplementary Data from Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance
Supplementary Data from Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance Open
Supplementary Data including Table S1-Table S5 and Figure S1 - Figure S9
View article: CD-20-0142R1_Supplementary_Table_S5.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S5.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S5
View article: Supplementary Figure S2: Western blot analysis of MAPK pathway inhibition by BI 847325 in BRAF-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S2: Western blot analysis of MAPK pathway inhibition by BI 847325 in BRAF-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
(A), MEK1 and phospho-MEK1/2; (B) ERK1/2 and phospho-ERK1/2.
View article: CD-20-0142R1_Supplementary_Table_S2.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S2.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S2
View article: Supplementary Data from Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance
Supplementary Data from Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance Open
Supplementary Data including Table S1-Table S5 and Figure S1 - Figure S9
View article: Data from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
Data from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
KRAS is the most frequently mutated driver of pancreatic, colorectal, and non–small cell lung cancers. Direct KRAS blockade has proved challenging, and inhibition of a key downstream effector pathway, the RAF–MEK–ERK cascade, has shown lim…
View article: CD-20-0142R1_Supplementary_Table_S2.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S2.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S2
View article: CD-20-0142R1_Supplementary_Table_S4.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S4.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S4
View article: Data from Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance
Data from Selective and Potent CDK8/19 Inhibitors Enhance NK-Cell Activity and Promote Tumor Surveillance Open
Natural killer (NK) cells play a pivotal role in controlling cancer. Multiple extracellular receptors and internal signaling nodes tightly regulate NK activation. Cyclin-dependent kinases of the mediator complex (CDK8 and CDK19) were descr…
View article: Supplementary Figure S3: Western blot analysis of MAPK pathway inhibition by BI 847325 in NRAS-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S3: Western blot analysis of MAPK pathway inhibition by BI 847325 in NRAS-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
(A), MEK1 and phospho-MEK1/2; (B) ERK1/2 and phospho-ERK1/2.
View article: Supplementary Figure S4: Western blot analysis of MAPK pathway inhibition by BI 847325 in KRAS-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S4: Western blot analysis of MAPK pathway inhibition by BI 847325 in KRAS-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
(A), MEK1 and phospho-MEK1/2; (B) ERK1/2 and phospho-ERK1/2.
View article: Data from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
Data from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
KRAS is the most frequently mutated driver of pancreatic, colorectal, and non–small cell lung cancers. Direct KRAS blockade has proved challenging, and inhibition of a key downstream effector pathway, the RAF–MEK–ERK cascade, has shown lim…
View article: Supplementary Figure S5: Efficacy of BI 847325 in the MIAPaCa-2 (KRASG12C) model of human pancreatic adenocarcinoma. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S5: Efficacy of BI 847325 in the MIAPaCa-2 (KRASG12C) model of human pancreatic adenocarcinoma. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
BomTac:NMRI-Foxn1nu mice bearing human MIAPaCa-2 tumors were treated with vehicle, BI 847325 at 10 mg/kg daily p.o., AZD6244 at 25 mg/kg twice daily p.o., GSK 1120212 at 0.25 mg/kg twice daily p.o. Data is plotted as average tumor volume w…
View article: Supplementary Figure S4: Western blot analysis of MAPK pathway inhibition by BI 847325 in KRAS-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Figure S4: Western blot analysis of MAPK pathway inhibition by BI 847325 in KRAS-mutant cell lines. from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
(A), MEK1 and phospho-MEK1/2; (B) ERK1/2 and phospho-ERK1/2.
View article: CD-20-0142R1_Supplementary_Table_S4.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S4.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S4
View article: CD-20-0142R1_Supplementary_Table_S9.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S9.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S9
View article: CD-20-0142R1_Supplementary_Table_S7.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S7.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S7
View article: CD-20-0142R1_Supplementary_Table_S5.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Table_S5.xlsx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Table S5
View article: CD-20-0142R1_Supplementary_Figures_S1-S5.docx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition
CD-20-0142R1_Supplementary_Figures_S1-S5.docx from BI-3406, a Potent and Selective SOS1–KRAS Interaction Inhibitor, Is Effective in KRAS-Driven Cancers through Combined MEK Inhibition Open
Supplementary Figures S1-S5
View article: Supplementary Table S1, S2, S3, S4 and Supplementary Figure legends from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases
Supplementary Table S1, S2, S3, S4 and Supplementary Figure legends from Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases Open
Supplementary Table S1: Statistics of data collection and processing of AuroraB/INCENP in complex with BI 847325; Supplementary Table S2: Statistics of data collection and processing of MEK1 in complex with BI 847325; Supplementary Table S…