Edith Ross
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View article: Figure 4 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Figure 4 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Dose- and exposure-dependent inhibition of KIT autophosphorylation with M4205 in the GIST430/654 model. A, Tumor-bearing mice were treated daily with three different doses of M4205 for 5 days, and inhibition of KIT autophosphorylation comp…
View article: Supplementary Table S6 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S6 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Cellular viability inhibition
View article: Supplementary Table S3 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S3 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
GENIE KIT mutation frequency
View article: Supplementary Table S1 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S1 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Animal model information
View article: Figure 1 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Figure 1 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Discovery of M4205, a potent inhibitor of disease-relevant KIT-mutant variants. A, Schematic overview of clinically observed mutations in different domains of the RTK KIT and estimated target coverage (green: positive; red: negative) of ap…
View article: Supplementary Table S10 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S10 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Split of M4205 concentration and FLT3 inhibition
View article: Supplementary Figure S2 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S2 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Cellular P-ERK1/2 and P-AKT inhibition
View article: Supplementary Table S2 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S2 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
In vivo formulation and administration
View article: Supplementary Figure S5 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S5 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Tolerability in mice
View article: Supplementary Table S4 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S4 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Biochemical inhibition of KIT variants
View article: Data from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Data from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Primary activating mutations in KIT (exon 9/11) are key driver alterations in about 80% of gastrointestinal stromal tumors (GIST). Imatinib, a small-molecule tyrosine kinase inhibitor, is used successfully as first-line therapy for patient…
View article: Figure 5 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Figure 5 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
In vivo antitumor activity of M4205 in xenograft models expressing oncogenic KIT mutations. Tumor bearing mice were treated daily with M4205 by oral gavage at doses indicated (10 mice per group). Body weight of mice was measured daily, and…
View article: Supplementary Figure S6 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S6 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
In vivo efficacy of SoC drugs
View article: Figure 6 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Figure 6 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Long-lasting antitumor effect under treatment with M4205 in a GIST PDX model with a KIT exon 11 mutation. Mice bearing a GIST PDX model with a KIT exon11 mutation (GS11328 WK557del) were treated continuously for 160 days once daily with M4…
View article: Supplementary Table S5 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S5 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Cellular P-KIT inhibition
View article: Figure 3 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Figure 3 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Cellular activity of M4205 compared with clinically approved KIT inhibitors. A–C, M4205 is more potent than imatinib, sunitinib, and ripretinib in inhibiting autophosphorylation (Y703) of KIT in GIST430 (KIT exon 11 del560-576), GIST430/65…
View article: Supplementary Figure S1 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S1 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Kinome Selectivity
View article: Supplementary Table S8 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S8 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Mouse Hematology
View article: Supplementary Table S7 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S7 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Mouse Histopathology
View article: Supplementary Table S9 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Table S9 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Mouse Clinical Chemistry
View article: Figure 2 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Figure 2 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Kinome selectivity of M4205. A, Selectivity of M4205 in the HotSpot kinase profiling panel (Reaction Biology) compared with approved and investigational KIT inhibitors at 1 μmol/L. The dots are scaled to the inhibition of the corresponding…
View article: Supplementary Figure S3 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S3 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Cell line viability screen
View article: Supplementary Figure S7 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S7 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Mouse PK and human dose prediction
View article: Supplementary Figure S4 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
Supplementary Figure S4 from M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
In vivo P-KIT and P-ERK1/2 inhibition
View article: M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer
M4205 (IDRX-42) Is a Highly Selective and Potent Inhibitor of Relevant Oncogenic Driver and Resistance Variants of KIT in Cancer Open
Primary activating mutations in KIT (exon 9/11) are key driver alterations in about 80% of gastrointestinal stromal tumors (GIST). Imatinib, a small-molecule tyrosine kinase inhibitor, is used successfully as first-line therapy for patient…
View article: Preclinical evidence for the effective use of TL-895, a highly selective and potent second-generation BTK inhibitor, for the treatment of B-cell malignancies
Preclinical evidence for the effective use of TL-895, a highly selective and potent second-generation BTK inhibitor, for the treatment of B-cell malignancies Open
TL-895 (formerly known as M7583) is a potent, highly selective, adenosine triphosphate (ATP)-competitive, second-generation, irreversible inhibitor of Bruton’s tyrosine kinase (BTK). We characterized its biochemical and cellular effects in…
View article: Additional file 7 of CONET: copy number event tree model of evolutionary tumor history for single-cell data
Additional file 7 of CONET: copy number event tree model of evolutionary tumor history for single-cell data Open
Additional file 7 Table S4 Assessment of CN calling for biological data.
View article: Additional file 6 of CONET: copy number event tree model of evolutionary tumor history for single-cell data
Additional file 6 of CONET: copy number event tree model of evolutionary tumor history for single-cell data Open
Additional file 6 Table S3 Assessment of CONET inference for biological data.
View article: Additional file 4 of CONET: copy number event tree model of evolutionary tumor history for single-cell data
Additional file 4 of CONET: copy number event tree model of evolutionary tumor history for single-cell data Open
Additional file 4 Table S1 Assessment of CONET accuracy and computational time for increasing number of cells.