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Therapy Name | G007-LK |
Synonyms | |
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, PMID: 32575464). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
G007-LK | Tankyrase Inhibitor 11 | 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, PMID: 32575464). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
APC dec exp | colorectal cancer | predicted - sensitive | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment altered gene expression pattern and induced growth arrest in intestinal organoids established from mouse models of colorectal cancer driven by APC knockdown, decreased proliferation and promoted differentiation in APC knockdown mouse models (PMID: 31337618). | 31337618 |
APC I1287Rfs*3 | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC I1287Rfs*3 in culture (PMID: 37968472). | 37968472 |
APC Y935* APC L1489Yfs*18 | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC L1489Yfs*18 and Y935* in culture (PMID: 37968472). | 37968472 |
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 Q886* | colorectal cancer | conflicting | G007-LK | Preclinical - Patient cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC Q886* in culture (PMID: 37968472). | 37968472 |
APC Q886* | colorectal cancer | conflicting | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment did not alter gene expression pattern or affect growth in mouse intestinal organoids expressing APC Q884* (corresponding to Q886* in human) in culture (PMID: 31337618). | 31337618 |
APC L1489* | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC L1489* in culture (PMID: 37968472). | 37968472 |
APC S299Tfs*7 APC R805* | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC R805* and S299Tfs*7 in culture (PMID: 37968472). | 37968472 |
APC L954* | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC L954* in culture (PMID: 37968472). | 37968472 |
APC E633* APC E1494* APC Q1529* | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC E1494*, E633*, and Q1529* in culture (PMID: 37968472). | 37968472 |
APC L852* | colorectal cancer | predicted - resistant | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment did not alter gene expression pattern or affect growth in intestinal organoids established from mouse models of colorectal cancer driven by APC L850* (corresponding to L852* in human), and had no effect on tumor cell growth and differentiation in APC L850* mouse models (PMID: 31337618). | 31337618 |
APC L1302Rfs*3 | colorectal cancer | resistant | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, a patient-derived colorectal cancer cell line harboring APC L1302Rfs*3 was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). | 37968472 |
APC G1116Efs*6 | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC G1116Efs*6 in culture (PMID: 37968472). | 37968472 |
APC S1356* | colorectal cancer | sensitive | G007-LK | Preclinical - Patient cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC S1356* in culture (PMID: 37968472). | 37968472 |
APC L665Ifs*8 APC R1450* | colorectal cancer | resistant | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, a patient-derived colorectal cancer cell line harboring APC L665Ifs*8 and R1450* was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). | 37968472 |
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 |
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 Q1367* | colorectal cancer | resistant | G007-LK | Preclinical - Patient cell culture | Actionable | In a preclinical study, a patient-derived colorectal cancer cell line harboring APC Q1367* was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). | 37968472 |
APC R499* | colorectal cancer | sensitive | G007-LK | Preclinical - Patient cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC R499* in culture (PMID: 37968472). | 37968472 |
APC Q1378* | colorectal cancer | sensitive | G007-LK | Preclinical - Patient cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC Q1378* in culture (PMID: 37968472). | 37968472 |
APC V830Gfs*12 APC T1556Nfs*3 | colorectal cancer | resistant | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, a patient-derived colorectal cancer cell line harboring APC V830Gfs*12 and T1556Nfs*3, along with PIK3CA E542K, was resistant to G007-LK treatment, as demonstrated by failure to inhibit viability in culture (PMID: 37968472). | 37968472 |
APC S1465Wfs*3 APC T1556Nfs*3 | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC S1465Wfs*3 and T1556Nfs*3 in culture (PMID: 37968472). | 37968472 |
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 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 E582fs | colorectal cancer | predicted - resistant | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment did not inhibit growth of mouse intestinal organoids expressing APC E580fs (corresponding to E582fs in human) in culture (PMID: 31337618). | 31337618 |
APC R876* | colorectal cancer | sensitive | G007-LK | Preclinical - Patient cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC R876* in culture (PMID: 37968472). | 37968472 |
APC R499* APC E1295* | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC E1295* and R499* in culture (PMID: 37968472). | 37968472 |
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 |
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 K670* | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC K670* in culture (PMID: 37968472). | 37968472 |
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 S1421Rfs*52 | colorectal cancer | sensitive | G007-LK | Preclinical - Cell culture | Actionable | In a preclinical study, G007-LK inhibited viability of a patient-derived colorectal cancer cell line harboring APC S1421Rfs*52 in culture (PMID: 37968472). | 37968472 |
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 |
CTNNB1 S33F | colorectal cancer | predicted - resistant | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment did not alter gene expression pattern or affect growth in mouse intestinal organoids expressing CTNNB1 S33F (corresponding to S33F in human) in culture (PMID: 31337618). | 31337618 |
APC Q1406* | colorectal cancer | predicted - sensitive | G007-LK | Preclinical | Actionable | In a preclinical study, G007-LK treatment altered gene expression pattern and inhibited growth of mouse intestinal organoids expressing APC Q1045* (corresponding to Q1046* in human) in culture (PMID: 31337618). | 31337618 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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