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FGFR2 (C491A/V564L)

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FGFR2 · Variant type: compound · HGVS: p.C491A;p.V564L

Components

p.C491Ap.V564L

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Pralsetinib100.0%0.0%93.43
2Entrectinib97.3%2.7%93.69
3Selpercatinib96.8%3.2%96.72
4Fedratinib95.9%4.1%96.21
5Defactinib95.2%4.8%92.68
6Sunitinib94.8%5.2%91.73
7Repotrectinib92.3%7.7%84.21
8Erdafitinib87.0%13.1%95.71
9Upadacitinib82.3%17.7%97.98
10Avapritinib78.5%21.6%97.73
11Pacritinib76.3%23.7%88.64
12Pemigatinib76.2%23.8%98.23
13Alpelisib72.8%27.2%97.22
14Gilteritinib66.0%34.0%88.97
15Tivozanib64.8%35.2%92.42
16Tenalisib63.8%36.2%97.98
17Pexidartinib57.9%42.1%99.49
18Infigratinib40.2%59.8%98.24
19Rabusertib39.3%60.7%98.74
20Deucravacitinib34.5%65.5%98.99
21Neratinib31.4%68.6%93.18
22Futibatinib27.7%72.3%98.48
23Darovasertib27.5%72.5%96.99
24Ripretinib20.9%79.1%92.95
25Tepotinib17.9%82.1%99.75

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)
Pralsetinib100.0%93.2%+6.8%
Entrectinib97.3%81.5%+15.7%
Selpercatinib96.8%95.0%+1.8%
Fedratinib95.9%
Defactinib95.2%
Sunitinib94.8%
Repotrectinib92.3%79.8%+12.5%
Erdafitinib87.0%99.0%-12.0%
Upadacitinib82.3%
Avapritinib78.5%
Pacritinib76.3%
Pemigatinib76.2%98.7%-22.6%
Alpelisib72.8%98.9%-26.2%
Gilteritinib66.0%
Tivozanib64.8%
Tenalisib63.8%96.0%-32.2%
Pexidartinib57.9%
Infigratinib40.2%98.8%-58.6%
Rabusertib39.3%
Deucravacitinib34.5%92.5%-58.0%
Neratinib31.4%
Futibatinib27.7%99.3%-71.6%
Darovasertib27.5%
Ripretinib20.9%85.4%-64.5%
Tepotinib17.9%

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