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CancerTools Org hct 116 brca2
Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 <t>BRCA2–/–</t> cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.
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Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 <t>BRCA2–/–</t> cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.
Hct116 Brca2, supplied by ATCC, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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CancerTools Org hct 116
Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 <t>BRCA2–/–</t> cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.
Hct 116, supplied by CancerTools Org, used in various techniques. Bioz Stars score: 93/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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European Collection of Authenticated Cell Cultures hct-116 (brca2− / − ) cell line
Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 <t>BRCA2–/–</t> cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.
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CancerTools Org hct 116 brca2 -/- 46
Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 <t>BRCA2–/–</t> cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.
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CancerTools Org hct 116 brca2 -/- 42
Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 <t>BRCA2–/–</t> cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.
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ATCC cell lines hct116 brca2
Table 1
Cell Lines Hct116 Brca2, supplied by ATCC, used in various techniques. Bioz Stars score: 99/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 BRCA2–/– cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.

Journal: Journal of Medicinal Chemistry

Article Title: RTx-303, an Orally Bioavailable Polθ Polymerase Inhibitor That Potentiates PARP Inhibitors in BRCA Mutant Tumors

doi: 10.1021/acs.jmedchem.5c00551

Figure Lengend Snippet: Cellular and in vitro activity of RTx-284. A. Bar plot showing the IC50 of RTx-284 in the indicated HR-proficient (gray) and HRD (red) cell lines. Data represent mean of at least 3 independent experiments performed in triplicate. B-D. Synergy plots created by Combenefit showing synergistic activity between RTx-284 and indicated PARPi in the indicated HRD cell lines. E. Bar plot showing that 10 μM RTx-284 suppresses the MMEJ GFP reporter. Data represent mean of 3 individual experiments performed in triplicate ±SEM. F. Dot plot showing increase of γH2AX following RTx-284:olaparib treatment in DLD1 BRCA2–/– cells. G. Bar plot showing that RTx-284 promotes an increase in caspase positive DLD1 BRCA2–/– cells. Data represent mean of 3 independent experiments performed in triplicate, ±SEM.

Article Snippet: HCT 116 BRCA2 −/– and HCT 116 Parental were obtained from Cancertools, London, UK.

Techniques: In Vitro, Activity Assay

RTx-303 potentiates PARPi in BRCA mutant cells and xenografts. A. Scatter plot showing relative viability of the indicated ID8 cells treated with the indicated concentrations of olaparib with and without 5 μM RTx-303. Data represent mean of 3 independent experiments performed in triplicate, ±SEM. B. Scatter plot showing BRCA2 mutant BR-05–0566 PDX volumes following treatment with vehicle, 45 mg/kg olaparib (PO,QD), 60 mg/kg RTx-303 (PO,BID), and 45 mg/kg olaparib (PO,QD) with 60 mg/kg RTx-303 (PO,BID) (left). Scatter plot showing % body weight change (right). Data represent mean, n = 7 ±SEM. C. Scatter plot showing BRCA2 mutant BR-05–0568 PDX volumes following treatment with vehicle, 0.12 mg/kg talazoparib (PO,QD) with and without 60 mg/kg RTx-303 (PO,BID) (left). Scatter plot showing % body weight change. (right). Data represent mean, n = 6 ±SEM. D. Scatter plot showing MDA-MB-436 tumor volumes following treatment with vehicle, 45 mg/kg olaparib (PO,QD) with and without 60 mg/kg RTx-303 (PO,BID) (left). Scatter plot showing % body weight change (right). Data represent mean, n = 8 ±SEM. * p < 0.05, *** p < 0.001.

Journal: Journal of Medicinal Chemistry

Article Title: RTx-303, an Orally Bioavailable Polθ Polymerase Inhibitor That Potentiates PARP Inhibitors in BRCA Mutant Tumors

doi: 10.1021/acs.jmedchem.5c00551

Figure Lengend Snippet: RTx-303 potentiates PARPi in BRCA mutant cells and xenografts. A. Scatter plot showing relative viability of the indicated ID8 cells treated with the indicated concentrations of olaparib with and without 5 μM RTx-303. Data represent mean of 3 independent experiments performed in triplicate, ±SEM. B. Scatter plot showing BRCA2 mutant BR-05–0566 PDX volumes following treatment with vehicle, 45 mg/kg olaparib (PO,QD), 60 mg/kg RTx-303 (PO,BID), and 45 mg/kg olaparib (PO,QD) with 60 mg/kg RTx-303 (PO,BID) (left). Scatter plot showing % body weight change (right). Data represent mean, n = 7 ±SEM. C. Scatter plot showing BRCA2 mutant BR-05–0568 PDX volumes following treatment with vehicle, 0.12 mg/kg talazoparib (PO,QD) with and without 60 mg/kg RTx-303 (PO,BID) (left). Scatter plot showing % body weight change. (right). Data represent mean, n = 6 ±SEM. D. Scatter plot showing MDA-MB-436 tumor volumes following treatment with vehicle, 45 mg/kg olaparib (PO,QD) with and without 60 mg/kg RTx-303 (PO,BID) (left). Scatter plot showing % body weight change (right). Data represent mean, n = 8 ±SEM. * p < 0.05, *** p < 0.001.

Article Snippet: HCT 116 BRCA2 −/– and HCT 116 Parental were obtained from Cancertools, London, UK.

Techniques: Mutagenesis

Table 1

Journal: The Journal of pathology

Article Title: Up-regulation of the interferon-related genes in BRCA2 knockout epithelial cells

doi: 10.1002/path.4404

Figure Lengend Snippet: Table 1

Article Snippet: Cell lines HCT116 BRCA2 +/+ cells were from ATCC (CCL-247), and the BRCA2 −/− cells were created in this study.

Techniques: