Therapy Detail

Therapy Name G007-LK
Synonym
Therapy Description

G007-LK inhibits tankyrase, which leads to stabilization of AXIN, thereby resulting in degradation of beta-catenin and decreased growth of APC-deficient tumors (PMID: 23539443).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
G007-LK Tankyrase Inhibitor 9 G007-LK inhibits tankyrase, which leads to stabilization of AXIN, thereby resulting in degradation of beta-catenin and decreased growth of APC-deficient tumors (PMID: 23539443).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
APC S811* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, treatment with G007-LK decreased active beta-catenin levels and Tcf/LEF activity, and reduced growth of a colorectal cancer cell line harboring APC S811* in culture (PMID: 28179481). 28179481
APC W553* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, G007-LK inhibited growth of a patient-derived colorectal cancer cell line harboring APC W553* in culture (PMID: 28179481). 28179481
APC S1197* APC S1278* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, treatment with G007-LK decreased active beta-catenin levels and Tcf/LEF activity, and reduced growth of a colorectal cancer cell line harboring APC S1197* and APC S1278* in culture (PMID: 28179481). 28179481
APC N1819fs APC wild-type colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring APC N1819fs (reported as N1819fs*7) and a wild-type copy of APC demonstrated low levels of Tcf/LEF activity, and was resistant to treatment with G007-LK in culture (PMID: 28179481). 28179481
APC R216* colorectal cancer sensitive G007-LK Preclinical - Cell culture Actionable In a preclinical study, a patient-derived colorectal cancer cell line harboring APC R216* demonstrated sensitivity to G007-LK in culture (PMID: 28179481). 28179481
Unknown unknown gastrointestinal stromal tumor not applicable G007-LK Preclinical Actionable In a preclinical study, G007-LK demonstrated anti-tumor activity in a mouse model of gastrointestinal stromal tumor expressing Kit V558del (corresponding to human V559del) (PMID: 28611108). 28611108
APC L665* APC R1450* colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring APC L665* and APC R1450* demonstrated low levels of Tcf/LEF activity, and was resistant to treatment with G007-LK in culture (PMID: 28179481). 28179481
APC I1164fs colorectal cancer sensitive G007-LK Preclinical - Patient cell culture Actionable In a preclinical study, G007-LK inhibited growth of a patient-derived colorectal cancer cell line harboring APC I1164fs in culture (PMID: 28179481). 28179481
APC E853* APC T1556fs colorectal cancer resistant G007-LK Preclinical - Cell culture Actionable In a preclinical study, a colorectal cancer cell line harboring APC E853* and APC T1556fs (reported as APC T1556fs*3) demonstrated low levels of Tcf/LEF activity, and was resistant to treatment with G007-LK in culture (PMID: 28179481). 28179481
APC inact mut colon cancer sensitive G007-LK Preclinical - Cell line xenograft Actionable In a preclinical study, G007-LK inhibited growth of APC-mutant colorectal cancer cell lines in culture and in xenograft models (PMID: 23539443). 23539443
Clinical Trial Phase Therapies Title Recruitment Status