Therapy Detail

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Therapy Name AZD1480
Synonyms
Therapy Description

AZD1480 is an ATP-competitive inhibitor of JAK1 and JAK2, which reduces STAT3 activation, potentially resulting in decreased tumor growth (PMID: 22027691, PMID: 24158701).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
AZD1480 AZD-1480 JAK1 Inhibitor - ATP competitive 4 JAK2 Inhibitor - ATP competitive 14 AZD1480 is an ATP-competitive inhibitor of JAK1 and JAK2, which reduces STAT3 activation, potentially resulting in decreased tumor growth (PMID: 22027691, PMID: 24158701) and has been also shown to inhibit ALK, LTK, FGFR1-3, RET and TRKA-C kinases (PMID: 29312610).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
JAK2 V617F JAK2 G935R hematologic cancer resistant AZD1480 Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 G935R double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). 21926964
JAK2 V617F JAK2 Y931C hematologic cancer resistant AZD1480 Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 Y931C double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). 21926964
CSF3R Q741* hematologic cancer predicted - sensitive AZD1480 Preclinical - Cell culture Actionable In a preclinical study, transformed hematologic cells expressing CSF3R Q741* were sensitive to treatment with AZD1480 in culture, demonstrating decreased cell survival (PMID: 28031554). 28031554
RET M918T thyroid gland medullary carcinoma sensitive AZD1480 Preclinical - Cell culture Actionable In a preclinical study, AZD1480 reduced phosphorylation of RET and downstream effectors, and inhibited growth and increased apoptosis of a medullary thyroid cancer cell line harboring RET M918T in culture (PMID: 23056499). 23056499
CEBPA mutant acute myeloid leukemia predicted - sensitive AZD1480 Preclinical - Patient cell culture Actionable In a preclinical study, patient-derived acute myeloid leukemia (AML) cells harboring biallelic CEBPA mutations demonstrated increased sensitivity to AZD1480 compared to control AML cells in culture (PMID: 27034432). 27034432
CSF3R T618I CSF3R Q741* hematologic cancer predicted - resistant AZD1480 Preclinical - Cell culture Actionable In a preclinical study, transformed hematologic cells co-expressing CSF3R T618I and CSF3R Q741* were resistant to treatment with AZD1480 in culture (PMID: 28031554). 28031554
RET C634W thyroid gland cancer sensitive AZD1480 Preclinical - Cell culture Actionable In a preclinical study, AZD1480 reduced phosphorylation of RET and downstream effectors, and inhibited growth and increased apoptosis of a thyroid cancer cell line harboring RET C634W in culture (PMID: 23056499). 23056499
JAK2 V617F JAK2 I960V hematologic cancer resistant AZD1480 Preclinical Actionable In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 I960V double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). 21926964
JAK2 V617F JAK2 E985K hematologic cancer resistant AZD1480 Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 E985K double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). 21926964
CSF3R T618I CSF3R W791* hematologic cancer predicted - resistant AZD1480 Preclinical - Cell culture Actionable In a preclinical study, transformed hematologic cells co-expressing CSF3R T618I and CSF3R W791* were resistant to treatment with AZD1480 in culture (PMID: 28031554). 28031554
JAK2 V617F JAK2 M929I hematologic cancer predicted - sensitive AZD1480 Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 M929I double mutation were sensitive to treatment with AZD1480 in culture, demonstrating growth inhibition (PMID: 21926964). 21926964
CSF3R W791* hematologic cancer predicted - sensitive AZD1480 Preclinical - Cell culture Actionable In a preclinical study, transformed hematologic cells expressing CSF3R W791** were sensitive to treatment with AZD1480 in culture, demonstrating decreased cell survival (PMID: 28031554). 28031554
JAK2 V617F JAK2 R938L hematologic cancer resistant AZD1480 Preclinical Actionable In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 R938L double mutation demonstrated resistance to AZD1480 in culture (PMID: 21926964). 21926964
Unknown unknown ovarian cancer not applicable AZD1480 Preclinical Actionable In a preclinical study, AZD1480 inhibited cell proliferation of ovarian cancer cells with active Jak-Stat signaling in culture and blocked tumor growth in transgenic mouse models of ovarian cancer (PMID: 25646015). 25646015

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Clinical Trial Phase Therapies Title Recruitment Status


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