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FGFR2 (C491A/V564I)

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FGFR2 · Variant type: compound · HGVS: p.C491A;p.V564I

Components

p.C491Ap.V564I

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Erdafitinib99.3%0.7%95.71
2Selpercatinib96.7%3.3%96.72
3Pemigatinib94.5%5.5%98.23
4Pralsetinib91.8%8.2%93.43
5Deucravacitinib86.6%13.4%98.99
6Pacritinib73.0%27.0%88.64
7Repotrectinib70.6%29.4%84.21
8Entrectinib69.0%31.0%93.69
9Fedratinib67.1%32.9%96.21
10Sunitinib65.3%34.7%91.73
11Infigratinib62.5%37.5%98.24
12Defactinib58.1%41.9%92.68
13Gilteritinib56.0%44.0%88.97
14Tepotinib55.6%44.4%99.75
15Avapritinib55.5%44.5%97.73
16Tivozanib54.3%45.7%92.42
17Tenalisib38.2%61.8%97.98
18Pexidartinib33.1%66.9%99.49
19Alpelisib31.6%68.4%97.22
20Upadacitinib30.3%69.7%97.98
21Sorafenib28.9%71.1%96.72
22Futibatinib24.6%75.4%98.48
23Canertinib19.7%80.3%96.49
24Erlotinib18.7%81.3%99.75
25Darovasertib17.1%82.9%96.99

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)
Erdafitinib99.3%99.0%+0.3%
Selpercatinib96.7%95.0%+1.7%
Pemigatinib94.5%98.7%-4.3%
Pralsetinib91.8%93.2%-1.4%
Deucravacitinib86.6%92.5%-5.9%
Pacritinib73.0%
Repotrectinib70.6%79.8%-9.2%
Entrectinib69.0%81.5%-12.6%
Fedratinib67.1%
Sunitinib65.3%
Infigratinib62.5%98.8%-36.4%
Defactinib58.1%
Gilteritinib56.0%
Tepotinib55.6%
Avapritinib55.5%
Tivozanib54.3%
Tenalisib38.2%96.0%-57.8%
Pexidartinib33.1%
Alpelisib31.6%98.9%-67.3%
Upadacitinib30.3%
Sorafenib28.9%
Futibatinib24.6%99.3%-74.7%
Canertinib19.7%
Erlotinib18.7%
Darovasertib17.1%

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