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AXL (R499C)

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AXL · Variant type: point · HGVS: p.R499C

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Gilteritinib98.0%2.0%88.97
2Cabozantinib95.9%4.1%92.73
3Neratinib94.1%5.9%93.18
4Crizotinib93.5%6.5%91.39
5Brigatinib93.5%6.5%82.96
6Sunitinib93.3%6.7%91.73
7Selpercatinib92.8%7.2%96.72
8Bosutinib88.5%11.5%87.22
9Pacritinib87.3%12.7%88.64
10Nintedanib87.0%13.0%90.23
11Alectinib85.3%14.7%95.49
12Pralsetinib81.1%18.9%93.43
13Lazertinib79.5%20.5%97.47
14Entrectinib79.4%20.6%93.69
15Fedratinib78.9%21.1%96.21
16Axitinib75.3%24.7%93.23
17Tivozanib74.2%25.8%92.42
18Repotrectinib69.6%30.4%84.21
19Tepotinib66.0%34.0%99.75
20Defactinib65.2%34.8%92.68
21Ponatinib60.5%39.5%78.23
22Fostamatinib59.9%40.1%96.74
23Vandetanib46.3%53.7%95.74
24Afatinib37.1%62.9%98.50
25Vemurafenib35.6%64.4%96.49

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)
Gilteritinib98.0%98.7%-0.7%
Cabozantinib95.9%95.9%-0.0%
Neratinib94.1%96.3%-2.2%
Crizotinib93.5%97.1%-3.6%
Brigatinib93.5%85.3%+8.2%
Sunitinib93.3%90.6%+2.8%
Selpercatinib92.8%85.2%+7.6%
Bosutinib88.5%89.9%-1.4%
Pacritinib87.3%89.8%-2.5%
Nintedanib87.0%79.5%+7.4%
Alectinib85.3%75.8%+9.5%
Pralsetinib81.1%76.7%+4.4%
Lazertinib79.5%81.1%-1.6%
Entrectinib79.4%73.6%+5.8%
Fedratinib78.9%76.3%+2.6%
Axitinib75.3%64.9%+10.4%
Tivozanib74.2%72.8%+1.4%
Repotrectinib69.6%77.8%-8.2%
Tepotinib66.0%69.6%-3.5%
Defactinib65.2%69.9%-4.7%
Ponatinib60.5%
Fostamatinib59.9%
Vandetanib46.3%
Afatinib37.1%
Vemurafenib35.6%

Cancer associations

CancerOrganSource
carcinoma_skinSkinref
carcinoma_large_intestineLarge Intestineref

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