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Ref Type Journal Article
PMID (21393331)
Authors Hornakova T, Springuel L, Devreux J, Dusa A, Constantinescu SN, Knoops L, Renauld JC
Title Oncogenic JAK1 and JAK2-activating mutations resistant to ATP-competitive inhibitors.
Journal Haematologica
Vol 96
Issue 6
Date 2011 Jun
URL
Abstract Text Activating mutations in JAK1 and JAK2 have been described in patients with various hematologic malignancies including acute lymphoblastic leukemia and myeloproliferative neoplasms, leading to clinical trials with JAK inhibitors. While there has been a tremendous effort towards the development of specific JAK inhibitors, mutations conferring resistance to such drugs have not yet been observed.Taking advantage of a model of spontaneous cellular transformation, we sequenced JAK1 in selected tumorigenic BaF3 clones and identified 25 de novo JAK1 activating mutations, including 5 mutations already described in human leukemias. We further used this library of JAK1 mutation-positive cell lines to assess their sensitivity to ATP-competitive inhibitors.While most JAK1 mutants were sensitive to ATP-competitive JAK inhibitors, mutations targeting Phe958 and Pro960 in the hinge region of the kinase domain rendered JAK1 constitutively active but also resistant to all tested JAK inhibitors. Furthermore, mutation of the homologous Tyr931 in JAK2 wild-type or JAK2 V617F mutant found in patients with myeloproliferative neoplasms also conferred resistance to JAK inhibitors, such as INCB018424, which is currently in clinical use.Our data indicate that some activating mutations not only promote autonomous cell proliferation but also confer resistance to ATP-competitive inhibitors. In vivo, such a mutation can potentially occur as primary JAK-activating mutations but also as secondary mutations combining oncogenicity with drug resistance.

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Molecular Profile Treatment Approach
JAK1 F734L JAK Inhibitor (Pan) - ATP competitive
JAK1 R724S JAK Inhibitor (Pan)
JAK1 Y654F JAK1 Inhibitor - ATP competitive
JAK1 K1026E JAK1 Inhibitor - ATP competitive
JAK1 K1026E JAK Inhibitor (Pan)
JAK1 G1097D JAK Inhibitor (Pan)
JAK1 Y654F JAK Inhibitor (Pan) - ATP competitive
JAK1 A634D JAK1 Inhibitor - ATP competitive
JAK1 K648N JAK Inhibitor (Pan) - ATP competitive
JAK1 F958V JAK Inhibitor (Pan)
JAK1 L710V JAK1 Inhibitor
JAK1 S1043I JAK Inhibitor (Pan) - ATP competitive
JAK1 T901R JAK Inhibitor (Pan)
JAK1 L783F JAK1 Inhibitor
JAK1 V658L JAK1 Inhibitor
JAK1 P960S JAK1 Inhibitor
JAK1 S703I JAK1 Inhibitor - ATP competitive
JAK1 Y654F JAK1 Inhibitor
JAK1 Y1035C JAK1 Inhibitor - ATP competitive
JAK1 L710V JAK1 Inhibitor - ATP competitive
JAK1 G1097D JAK Inhibitor (Pan) - ATP competitive
JAK1 R724S JAK1 Inhibitor - ATP competitive
JAK1 Y652H JAK1 Inhibitor
JAK1 E897K JAK1 Inhibitor
JAK1 L910Q JAK Inhibitor (Pan)
JAK1 F958L JAK1 Inhibitor
JAK1 V658F JAK1 Inhibitor - ATP competitive
JAK1 F734L JAK Inhibitor (Pan)
JAK1 S729C JAK Inhibitor (Pan)
JAK1 K1026E JAK1 Inhibitor
JAK1 K648N JAK1 Inhibitor - ATP competitive
JAK1 P815S JAK Inhibitor (Pan) - ATP competitive
JAK1 K1026E JAK Inhibitor (Pan) - ATP competitive
JAK1 F958L JAK Inhibitor (Pan)
JAK1 S646P JAK Inhibitor (Pan)
JAK1 L710V JAK Inhibitor (Pan) - ATP competitive
JAK1 R724H JAK1 Inhibitor
JAK1 D895H JAK Inhibitor (Pan) - ATP competitive
JAK1 F635V JAK Inhibitor (Pan)
JAK1 L910Q JAK1 Inhibitor - ATP competitive
JAK1 T901R JAK Inhibitor (Pan) - ATP competitive
JAK1 S646F JAK1 Inhibitor - ATP competitive
JAK1 A634D JAK Inhibitor (Pan)
JAK1 L783F JAK Inhibitor (Pan) - ATP competitive
JAK1 F958S JAK Inhibitor (Pan)
JAK1 F958C JAK Inhibitor (Pan)
JAK1 A723D JAK1 Inhibitor - ATP competitive
JAK1 R629_D630del JAK1 Inhibitor - ATP competitive
JAK1 A723D JAK Inhibitor (Pan)
JAK1 G1097D JAK1 Inhibitor
JAK1 P815S JAK Inhibitor (Pan)
JAK1 Y1035C JAK Inhibitor (Pan) - ATP competitive
JAK1 R724H JAK1 Inhibitor - ATP competitive
JAK1 S646P JAK Inhibitor (Pan) - ATP competitive
JAK1 V658F JAK Inhibitor (Pan)
JAK1 R724S JAK1 Inhibitor
JAK1 E897K JAK1 Inhibitor - ATP competitive
JAK1 K648N JAK Inhibitor (Pan)
JAK1 R629_D630del JAK Inhibitor (Pan) - ATP competitive
JAK1 A634D JAK Inhibitor (Pan) - ATP competitive
JAK1 R629_D630del JAK1 Inhibitor
JAK1 P815S JAK1 Inhibitor
JAK1 L910P JAK1 Inhibitor
JAK1 Y1035C JAK Inhibitor (Pan)
JAK1 P815S JAK1 Inhibitor - ATP competitive
JAK1 K648N JAK1 Inhibitor
JAK1 V658F JAK1 Inhibitor
JAK1 Y652H JAK Inhibitor (Pan) - ATP competitive
JAK1 D895H JAK1 Inhibitor
JAK1 S646P JAK1 Inhibitor - ATP competitive
JAK1 R629_D630del JAK Inhibitor (Pan)
JAK1 L783F JAK Inhibitor (Pan)
JAK1 A634D JAK1 Inhibitor
JAK1 R879H JAK1 Inhibitor - ATP competitive
JAK1 F958S JAK1 Inhibitor
JAK1 S703I JAK Inhibitor (Pan) - ATP competitive
JAK1 S1043I JAK1 Inhibitor
JAK1 F635V JAK1 Inhibitor
JAK1 V658L JAK1 Inhibitor - ATP competitive
JAK1 act mut JAK1 Inhibitor - ATP competitive
JAK1 V658L JAK Inhibitor (Pan)
JAK1 act mut JAK Inhibitor (Pan)
JAK1 S646F JAK1 Inhibitor
JAK1 S729C JAK1 Inhibitor
JAK1 L910P JAK Inhibitor (Pan)
JAK1 V658L JAK Inhibitor (Pan) - ATP competitive
JAK1 L910Q JAK1 Inhibitor
JAK1 V658I JAK1 Inhibitor - ATP competitive
JAK1 Y652H JAK Inhibitor (Pan)
JAK1 R879C JAK Inhibitor (Pan)
JAK1 F958V JAK1 Inhibitor
JAK1 F635V JAK Inhibitor (Pan) - ATP competitive
JAK1 D895H JAK Inhibitor (Pan)
JAK1 L910P JAK1 Inhibitor - ATP competitive
JAK1 R879H JAK Inhibitor (Pan)
JAK1 Y652H JAK1 Inhibitor - ATP competitive
JAK1 S1043I JAK Inhibitor (Pan)
JAK1 F734L JAK1 Inhibitor - ATP competitive
JAK1 Y654F JAK Inhibitor (Pan)
JAK1 S646F JAK Inhibitor (Pan) - ATP competitive
JAK1 P960T JAK Inhibitor (Pan)
JAK1 act mut JAK Inhibitor (Pan) - ATP competitive
JAK1 R879C JAK1 Inhibitor - ATP competitive
JAK1 Y1035C JAK1 Inhibitor
JAK1 S729C JAK1 Inhibitor - ATP competitive
JAK1 R879H JAK1 Inhibitor
JAK1 P960S JAK Inhibitor (Pan)
JAK1 R724S JAK Inhibitor (Pan) - ATP competitive
JAK1 R879C JAK1 Inhibitor
JAK1 F958C JAK1 Inhibitor
JAK1 E897K JAK Inhibitor (Pan)
JAK1 S646F JAK Inhibitor (Pan)
JAK1 T901R JAK1 Inhibitor - ATP competitive
JAK1 S703I JAK1 Inhibitor
JAK1 L783F JAK1 Inhibitor - ATP competitive
JAK1 E897K JAK Inhibitor (Pan) - ATP competitive
JAK1 V658I JAK Inhibitor (Pan) - ATP competitive
JAK1 S1043I JAK1 Inhibitor - ATP competitive
JAK1 F635V JAK1 Inhibitor - ATP competitive
JAK1 V658F JAK Inhibitor (Pan) - ATP competitive
JAK1 S729C JAK Inhibitor (Pan) - ATP competitive
JAK1 R724H JAK Inhibitor (Pan)
JAK1 D895H JAK1 Inhibitor - ATP competitive
JAK1 S703I JAK Inhibitor (Pan)
JAK1 S646P JAK1 Inhibitor
JAK1 A723D JAK Inhibitor (Pan) - ATP competitive
JAK1 G1097D JAK1 Inhibitor - ATP competitive
JAK1 act mut JAK1 Inhibitor
JAK1 L910P JAK Inhibitor (Pan) - ATP competitive
JAK1 A723D JAK1 Inhibitor
JAK1 R879C JAK Inhibitor (Pan) - ATP competitive
JAK1 P960T JAK1 Inhibitor
JAK1 L910Q JAK Inhibitor (Pan) - ATP competitive
JAK1 T901R JAK1 Inhibitor
JAK1 V658I JAK1 Inhibitor
JAK1 F734L JAK1 Inhibitor
JAK1 L710V JAK Inhibitor (Pan)
JAK1 V658I JAK Inhibitor (Pan)
JAK1 R879H JAK Inhibitor (Pan) - ATP competitive
JAK1 R724H JAK Inhibitor (Pan) - ATP competitive
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
JAK1 A723D missense gain of function JAK1 A723D lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). A723D results in constitutive phosphorylation of Jak1 and Stat5 in cell culture (PMID: 21393331, PMID: 24735922).
JAK1 D895H missense gain of function JAK1 D895H lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). D895H results in constitutive Jak1 phosphorylation, increased phosphorylation of Stat5 and Erk in culture, and tumor formation in mouse models (PMID: 21393331).
JAK1 E897K missense gain of function - predicted JAK1 E897K lies within the protein kinase domain 2 of the Jak1 protein (UniProt). E897K results in constitutive Jak1 phosphorylation, and increased phosphorylation of Stat5 and Erk in culture (PMID: 21393331), and therefore, is predicted to lead a gain of Jak1 protein function.
JAK1 F635V missense gain of function JAK1 F635V lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). F635V results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331).
JAK1 F734L missense gain of function - predicted JAK1 F734L lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). F734L results in constitutive Jak1 phosphorylation, and increased phosphorylation of Stat5 and Erk in culture (PMID: 21393331), and therefore, is predicted to lead a gain of Jak1 protein function.
JAK1 F958C missense gain of function JAK1 F958C lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). F958C results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, transformation of cultured cells, and confers resistance to Jak inhibitors in culture (PMID: 21393331). Y
JAK1 F958L missense gain of function - predicted JAK1 F958L lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). F958L results in constitutive Jak1 phosphorylation, increased phosphorylation of Stat5 and Erk in culture, and confers resistance to Jak inhibitors in culture (PMID: 21393331), and therefore, is predicted to lead to a gain of Jak1 protein function. Y
JAK1 F958S missense gain of function JAK1 F958S lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). F958S results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, transformation of cultured cells, and confers resistance to Jak inhibitors in culture (PMID: 21393331, PMID: 20868368). Y
JAK1 F958V missense gain of function JAK1 F958V lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). F958V results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, transformation of cultured cells, and tumor formation in mouse models, and confers resistance to Jak inhibitors in culture (PMID: 21393331). Y
JAK1 K1026E missense gain of function - predicted JAK1 K1026E lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). K1026E is transforming in culture and promotes tumor formation in mouse models, but results in variable phosphorylation levels of Jak1 and downstream signaling proteins in culture (PMID: 21393331, PMID: 20868368), and therefore, is predicted to lead to a gain of Jak1 protein function.
JAK1 L783F missense gain of function JAK1 L783F lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). Y652H results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331).
JAK1 L910Q missense gain of function - predicted JAK1 L910Q lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). L910Q results in constitutive Jak1 phosphorylation and increased phosphorylation of Stat5 in culture (PMID: 21393331), and therefore, is predicted to lead to a gain of Jak1 protein function.
JAK1 P815S missense gain of function JAK1 P815S lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). P815S results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331).
JAK1 P960S missense gain of function JAK1 P960S lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). P960S results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk (PMID: 21393331), transformation of cultured cells (PMID: 20868368), and confers resistance to Jak inhibitors in culture (PMID: 21393331).. Y
JAK1 P960T missense gain of function JAK1 P960T lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). P960T results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, transformation of cultured cells, and confers resistance to Jak inhibitors in culture (PMID: 21393331). Y
JAK1 R724S missense gain of function JAK1 R724S lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). R724S results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331).
JAK1 S1043I missense gain of function JAK1 S1043I lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). S1043I results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, transformation of cultured cells, and tumor formation in mouse models (PMID: 21393331).
JAK1 S646F missense gain of function JAK1 S646F lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). S646F results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331, PMID: 21551237).
JAK1 S703I missense gain of function JAK1 S703I lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). S703I results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 24825865, PMID: 21393331).
JAK1 T901R missense gain of function JAK1 T901R lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). T901R results in constitutive Jak1 phosphorylation, increased phosphorylation of Stat5 and Erk in culture (PMID: 21393331), and therefore, is predicted to lead a gain of Jak1 protein function.
JAK1 V658F missense gain of function JAK1 V658F lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). V658F results in constitutive Jak1 activation, increased ligand-independent phosphorylation of Stat1, Stat5, and Erk (PMID: 21393331, PMID: 31892268), transformation of cultured cells, and tumor formation in mouse models (PMID: 21393331).
JAK1 V658I missense gain of function JAK1 V658I lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). V658I results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331).
JAK1 V658L missense gain of function JAK1 V658L lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). V658L results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331, PMID: 20868368).
JAK1 Y1035C missense gain of function JAK1 Y1035C lies within the protein kinase domain 2 of the Jak1 protein (UniProt.org). Y1035C results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331, PMID: 20868368).
JAK1 Y652H missense gain of function JAK1 Y652H lies within the protein kinase domain 1 of the Jak1 protein (UniProt.org). Y652H results in constitutive Jak1 activation, increased phosphorylation of Stat5 and Erk, and is transforming in cell culture (PMID: 21393331, PMID: 21551237).
JAK2 Y931C missense gain of function JAK2 Y931C lies within the protein kinase domain 2 of the Jak2 protein (UniProt.org). Y931C results in increased phosphorylation of Jak2 and Stat5, is transforming in cell culture, and confers resistance to Jak inhibitors (PMID: 21393331, PMID: 26419724). Y
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
JAK2 V617F JAK2 Y931C cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring the JAK2 V617F/Y931C double mutation displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 P960S cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK1 P960S displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 K1026E cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 K1026E were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 F958C cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK1 F958C displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 Y1035C cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 Y1035C were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 T901R cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 T901R were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 P960T cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK1 P960T displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 V658F cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells expressing JAK1 V658F were sensitive to ATP-competitive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 V658I cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 V658I were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 R724S cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 R724S were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 S1043I cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 S1043I were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 F734L cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 F734L were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 F958L cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK1 F958L displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 S703I cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 S703I were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 V658L cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 V658L were sensitive to ATP-competetive JAK (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 Y652H cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 Y652H were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 E897K cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 E897K were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK2 Y931C cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK2 Y931C displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 V658F JAK1 F958C cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring the JAK1 V658F/F958C double mutation displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 L910Q cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 L910Q were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 F958S cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK1 F958S displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 L783F cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 L783F were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 S646F cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 S646F were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 A723D cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 A723D were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 P815S cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 P815S were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 F958V cancer resistant Ruxolitinib Preclinical Actionable In a preclinical study, cells harboring JAK1 F958V displayed resistance to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 D895H cancer sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 D895H were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331
JAK1 F635V Advanced Solid Tumor sensitive Ruxolitinib Preclinical Actionable In a preclinical study, transformed cells harboring JAK1 F635V were sensitive to ATP-competetive JAK inhibitors, such as Jakafi (Ruxolitinib) (PMID: 21393331). 21393331