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TIE2 (R915C)

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

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Repotrectinib83.3%16.7%84.21
2Ripretinib81.8%18.2%92.95
3Vandetanib55.0%45.0%95.74
4Infigratinib53.8%46.2%98.24
5Neratinib52.3%47.7%93.18
6Tivozanib50.3%49.7%92.42
7Pacritinib36.0%64.0%88.64
8Erdafitinib32.0%68.0%95.71
9Defactinib30.5%69.5%92.68
10Entrectinib25.4%74.6%93.69
11Apatinib17.3%82.7%97.73
12Selpercatinib17.0%83.0%96.72
13Pemigatinib15.5%84.5%98.23
14Umbralisib13.7%86.3%98.74
15Avapritinib13.7%86.3%97.73
16Fedratinib9.7%90.3%96.21
17Upadacitinib9.2%90.8%97.98
18Gilteritinib9.0%91.0%88.97
19Rabusertib8.8%91.2%98.74
20Canertinib8.8%91.2%96.49
21Inavolisib8.8%91.3%100.00
22Capivasertib7.6%92.4%96.48
23Asciminib6.5%93.5%100.00
24Pexidartinib6.1%93.9%99.49
25Acalabrutinib5.3%94.7%99.50

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)
Repotrectinib83.3%
Ripretinib81.8%
Vandetanib55.0%
Infigratinib53.8%
Neratinib52.3%
Tivozanib50.3%
Pacritinib36.0%
Erdafitinib32.0%
Defactinib30.5%
Entrectinib25.4%
Apatinib17.3%
Selpercatinib17.0%
Pemigatinib15.5%
Umbralisib13.7%
Avapritinib13.7%
Fedratinib9.7%
Upadacitinib9.2%
Gilteritinib9.0%
Rabusertib8.8%
Canertinib8.8%
Inavolisib8.8%
Capivasertib7.6%
Asciminib6.5%
Pexidartinib6.1%
Acalabrutinib5.3%

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