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View article: Supplementary Figure S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Figure S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Supplementary Figure 1. RLY-4008 is an irreversible inhibitor of FGFR2.
View article: Supplementary Table S3 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S3 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Antiproliferative effect of RLY-4008 and pan-FGFRi in human tumor cell lines
View article: Supplementary Table S4 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S4 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
In vivo exposures of pan-FGFRi in mouse studies
View article: Supplementary Table S5 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S5 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Fold change in potency against FGFR2 acquired resistance mutations
View article: Supplementary References from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary References from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
three references cited in supplementary data
View article: Supplementary Appendix S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Appendix S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
ReFocus entry criteria
View article: Supplementary Video S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Video S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
In this schematic movie, apo FGFR1 (left panel) demonstrates rapid P-loop dynamics, while apo FGFR2 (right panel) displays less P-loop motion.
View article: Supplementary Video S1 Legend from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Video S1 Legend from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Supplementary video legend describing schematic video of P-loop dynamics
View article: Supplementary Appendix S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Appendix S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
ReFocus entry criteria
View article: Supplementary Video S1 Legend from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Video S1 Legend from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Supplementary video legend describing schematic video of P-loop dynamics
View article: Supplementary Video S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Video S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
In this schematic movie, apo FGFR1 (left panel) demonstrates rapid P-loop dynamics, while apo FGFR2 (right panel) displays less P-loop motion.
View article: Supplementary Table S4 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S4 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
In vivo exposures of pan-FGFRi in mouse studies
View article: Supplementary Table S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Potency (kinact/KI) of RLY-4008 against FGFR1 and FGFR2
View article: Supplementary Table S3 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S3 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Antiproliferative effect of RLY-4008 and pan-FGFRi in human tumor cell lines
View article: Supplementary References from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary References from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
three references cited in supplementary data
View article: Supplementary Table S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Biochemical inhibition of FGFR by RLY-4008 and pan-FGFRi
View article: Supplementary Table S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Potency (kinact/KI) of RLY-4008 against FGFR1 and FGFR2
View article: Supplementary Figure S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Figure S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Supplementary Figure 2. Treatment with RLY-4008 is well-tolerated and leads to dose-dependent inhibition of FGFR2 and tumor regression in multiple FGFR2-altered tumor models.
View article: Supplementary Figure S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Figure S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Supplementary Figure 2. Treatment with RLY-4008 is well-tolerated and leads to dose-dependent inhibition of FGFR2 and tumor regression in multiple FGFR2-altered tumor models.
View article: Supplementary Table S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S2 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Biochemical inhibition of FGFR by RLY-4008 and pan-FGFRi
View article: Supplementary Figure S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Figure S1 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Supplementary Figure 1. RLY-4008 is an irreversible inhibitor of FGFR2.
View article: Data from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Data from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Oncogenic activation of fibroblast growth factor receptor 2 (FGFR2) drives multiple cancers and represents a broad therapeutic opportunity, yet selective targeting of FGFR2 has not been achieved. While the clinical efficacy of pan-FGFR inh…
View article: Supplementary Table S5 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations
Supplementary Table S5 from RLY-4008, the first highly selective FGFR2 inhibitor with activity across FGFR2 alterations and resistance mutations Open
Fold change in potency against FGFR2 acquired resistance mutations
View article: Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2
Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2 Open
Fibroblast growth factor receptor (FGFR) kinase inhibitors have been shown to be effective in the treatment of intrahepatic cholangiocarcinoma and other advanced solid tumors harboring FGFR2 alterations, but the toxicity of these drugs fre…
View article: Supplementary Table S1 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations
Supplementary Table S1 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations Open
Potency (kinact/KI) of RLY-4008 against FGFR1 and FGFR2
View article: Data from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations
Data from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations Open
Oncogenic activation of fibroblast growth factor receptor 2 (FGFR2) drives multiple cancers and represents a broad therapeutic opportunity, yet selective targeting of FGFR2 has not been achieved. Although the clinical efficacy of pan-FGFR …
View article: Supplementary Appendix S1 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations
Supplementary Appendix S1 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations Open
ReFocus entry criteria
View article: Supplementary References from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations
Supplementary References from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations Open
three references cited in supplementary data
View article: Supplementary Figure S1 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations
Supplementary Figure S1 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations Open
Supplementary Figure 1. RLY-4008 is an irreversible inhibitor of FGFR2.
View article: Supplementary Figure S2 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations
Supplementary Figure S2 from RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across <i>FGFR2</i> Alterations and Resistance Mutations Open
Supplementary Figure 2. Treatment with RLY-4008 is well-tolerated and leads to dose-dependent inhibition of FGFR2 and tumor regression in multiple FGFR2-altered tumor models.