Gene Variant Detail

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Gene PIK3CA
Variant K111N
Impact List missense
Protein Effect gain of function
Gene Variant Descriptions PIK3CA K111N lies within the region linking the PI3K-ABD and PI3K-RBD domains of the Pik3ca protein (UniProt.org). K111N results in increased phosphorylation of Akt, activation of downstream signaling, increased cell proliferation and migration, and is transforming in cell culture (PMID: 17376864, PMID: 29533785, PMID: 34779417).
Associated Drug Resistance
Category Variants Paths

PIK3CA mutant PIK3CA act mut PIK3CA K111N

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Transcript NM_006218.4
gDNA chr3:g.179199158G>C
cDNA c.333G>C
Protein p.K111N
Source Database RefSeq
Genome Build GRCh38/hg38
Transcript gDNA cDNA Protein Source Database Genome Build
XM_006713658 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
XM_006713658.4 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
NM_006218 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
XM_011512894 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
XM_006713658.5 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
NM_006218.3 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
NM_006218.4 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38
XM_011512894.2 chr3:g.179199158G>C c.333G>C p.K111N RefSeq GRCh38/hg38

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA K111N estrogen-receptor positive breast cancer sensitive AZD8835 Preclinical Actionable In a preclinical study, AZD8835 inhibited proliferation of estrogen receptor (ER)-positive breast cancer cells harboring PIK3CA K111N in culture and induced tumor regression in xenograft models (PMID: 26839307). 26839307
PIK3CA K111N breast cancer sensitive BAY1125976 Preclinical - Cell culture Actionable In a preclinical study, BAY1125976 inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 27699769). 27699769
PIK3CA K111N breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, hormone receptor positive breast cancer cells harboring PIK3CA K111N were sensitive to Miransertib (ARQ092) in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
PIK3CA K111N breast cancer sensitive Miransertib Preclinical - Cell culture Actionable In a preclinical study, Miransertib (ARQ092) treatment induced cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, a breast cancer cell line harboring PIK3CA K111N was sensitive to ARQ 751 in culture, demonstrating inhibition of cell growth (PMID: 26469692). 26469692
PIK3CA K111N breast cancer sensitive ARQ 751 Preclinical - Cell culture Actionable In a preclinical study, ARQ 751 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive DHM25 Preclinical - Cell culture Actionable In a preclinical study, DHM25 increased cell death in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 26237138). 26237138
PIK3CA K111N breast cancer sensitive Borussertib Preclinical - Cell culture Actionable In a preclinical study, borussertib inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 30858154). 30858154
PIK3CA K111N breast cancer sensitive MK2206 Preclinical - Cell culture Actionable In a preclinical study, MK2206 treatment increased cell death and inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer predicted - sensitive GSK690693 Preclinical - Cell culture Actionable In a preclinical study, GSK690693 treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer predicted - sensitive Ipatasertib Preclinical - Cell culture Actionable In a preclinical study, Ipatasertib (GDC-0068) treatment did not increase cell death but inhibited proliferation of a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive AZD0156 + Miransertib Preclinical - Cell culture Actionable In a preclinical study, AZD0156 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive KU-57788 + Miransertib Preclinical - Cell culture Actionable In a preclinical study, KU-57788 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive GSK2334470 + Miransertib Preclinical - Cell culture Actionable In a preclinical study, GSK2334470 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive Miransertib + OSU-T315 Preclinical - Cell culture Actionable In a preclinical study, OSU-T315 and Miransertib (ARQ092) combination treatment increased cell death compared to Miransertib (ARQ092) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive Ipatasertib + OSU-T315 Preclinical - Cell culture Actionable In a preclinical study, OSU-T315 and Ipatasertib (GDC0068) combination treatment increased cell death compared to Ipatasertib (GDC0068) alone in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 32439931). 32439931
PIK3CA K111N breast cancer sensitive MEN1611 Preclinical - Cell culture Actionable In a preclinical study, MEN1611 (CH5132799) inhibited viability in a breast cancer cell line harboring PIK3CA K111N in culture (PMID: 36913051). 36913051