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TIE2 (Y897H/R915C)

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TEK · Variant type: point · HGVS: p.R915C

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Repotrectinib64.5%35.5%84.21
2Ripretinib63.7%36.3%92.95
3Selpercatinib35.7%64.3%96.72
4Infigratinib23.7%76.3%98.24
5Tivozanib22.2%77.8%92.42
6Neratinib20.8%79.2%93.18
7Pemigatinib19.8%80.2%98.23
8Vandetanib19.4%80.6%95.74
9Pacritinib13.4%86.6%88.64
10Erdafitinib13.3%86.7%95.71
11Defactinib11.3%88.7%92.68
12Selumetinib8.0%92.0%100.00
13Pirtobrutinib7.6%92.4%99.49
14Mitapivat7.3%92.7%100.00
15Umbralisib7.3%92.7%98.74
16Cobimetinib6.7%93.3%100.00
17Gedatolisib6.4%93.6%99.75
18Mobocertinib4.9%95.1%97.22
19Abrocitinib4.4%95.6%99.50
20Apatinib4.4%95.6%97.73
21Tucatinib4.4%95.6%99.75
22Asciminib2.9%97.1%100.00
23Paxalisib2.6%97.4%99.75
24Sorafenib1.4%98.6%96.72
25Lazertinib0.8%99.2%97.47

Wild-type vs variant — drug response delta

Positive Δ means the drug hits the variant harder than wild-type (mutation-selective); negative Δ means it loses potency (resistance).

DrugVariant inhWT inhΔ (variant − WT)
Repotrectinib64.5%
Ripretinib63.7%
Selpercatinib35.7%
Infigratinib23.7%
Tivozanib22.2%
Neratinib20.8%
Pemigatinib19.8%
Vandetanib19.4%
Pacritinib13.4%
Erdafitinib13.3%
Defactinib11.3%
Selumetinib8.0%
Pirtobrutinib7.6%
Mitapivat7.3%
Umbralisib7.3%
Cobimetinib6.7%
Gedatolisib6.4%
Mobocertinib4.9%
Abrocitinib4.4%
Apatinib4.4%
Tucatinib4.4%
Asciminib2.9%
Paxalisib2.6%
Sorafenib1.4%
Lazertinib0.8%

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