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Gene | KIT |
Variant | D816H |
Impact List | missense |
Protein Effect | gain of function |
Gene Variant Descriptions | KIT D816H lies within the tyrosine kinase domain region 2 (exon 17) of the Kit protein (PMID: 19164557). D816H results in increased kinase activity, constitutive Kit phosphorylation, activation of Stat3 signaling, and transformation of cultured cells (PMID: 10362788, PMID: 11494148), and confers resistance to some Kit inhibitors (PMID: 25239608). |
Associated Drug Resistance | Y |
Category Variants Paths |
KIT mutant KIT act mut KIT D816H KIT mutant KIT exon17 KIT D816X KIT D816H |
Transcript | NM_000222.3 |
gDNA | chr4:g.54733154G>C |
cDNA | c.2446G>C |
Protein | p.D816H |
Source Database | RefSeq |
Genome Build | GRCh38/hg38 |
Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
---|---|---|---|---|---|
NM_000222.2 | chr4:g.54733154G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_000222 | chr4:g.54733154G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_001093772 | chr4:g.54733166G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_001093772.1 | chr4:g.54733166G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_001385292.1 | chr4:g.54733166G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
XM_005265741.1 | chr4:g.54733154G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_001093772.2 | chr4:g.54733166G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
XM_017008179 | chr4:g.54733166G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_001385290.1 | chr4:g.54733154G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
NM_000222.3 | chr4:g.54733154G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
XM_005265741 | chr4:g.54733154G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
XM_017008179.1 | chr4:g.54733166G>C | c.2446G>C | p.D816H | RefSeq | GRCh38/hg38 |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT D816H | Advanced Solid Tumor | resistant | Imatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816H were resistant to Gleevec (imatinib) treatment in culture (PMID: 35194937). | 35194937 |
KIT D816H | Advanced Solid Tumor | sensitive | Ponatinib | Preclinical | Actionable | In a preclinical study, cells expressing KIT D816H demonstrated sensitivity to Iclusig (ponatinib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT D816H | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, KIT D816H demonstrated resistance to Stivarga (regorafenib) in an in vitro assay, and conferred secondary resistance to Stivarga (regorafenib) in transformed cells expressing other KIT mutations (PMID: 25239608). | 25239608 |
KIT D816H | Advanced Solid Tumor | predicted - sensitive | Sunitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816H were more sensitive to treatment with Sutent (sunitinib) in culture compared to Gleevec (imatinib) (PMID: 24205792). | 24205792 |
KIT D816H | Advanced Solid Tumor | predicted - sensitive | Flumatinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816H were more sensitive to treatment with Flumatinib in culture compared to Gleevec (imatinib) (PMID: 24205792). | 24205792 |