TIE2 (Y897C)

TEK · Variant type: point · HGVS: p.Y897C

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Ponatinib	94.5%	5.5%	78.23
2	Ripretinib	92.8%	7.2%	92.95
3	Tivozanib	91.8%	8.2%	92.42
4	Repotrectinib	87.1%	12.9%	84.21
5	Cabozantinib	79.8%	20.2%	92.73
6	Erdafitinib	78.9%	21.1%	95.71
7	Crizotinib	78.1%	21.9%	91.39
8	Brigatinib	75.0%	25.0%	82.96
9	Pemigatinib	74.5%	25.5%	98.23
10	Neratinib	73.9%	26.1%	93.18
11	Selpercatinib	61.7%	38.3%	96.72
12	Axitinib	56.9%	43.1%	93.23
13	Infigratinib	56.2%	43.8%	98.24
14	Nintedanib	54.7%	45.3%	90.23
15	Vandetanib	51.4%	48.6%	95.74
16	Defactinib	48.0%	52.0%	92.68
17	Apatinib	37.5%	62.5%	97.73
18	Pacritinib	37.4%	62.6%	88.64
19	Umbralisib	35.8%	64.2%	98.74
20	Entrectinib	30.1%	69.9%	93.69
21	Canertinib	28.5%	71.5%	96.49
22	Bosutinib	25.0%	75.0%	87.22
23	Upadacitinib	22.0%	78.0%	97.98
24	Futibatinib	20.7%	79.3%	98.48
25	Regorafenib	17.9%	82.1%	95.99

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

Drug	Variant inh	WT inh	Δ (variant − WT)
Ponatinib	94.5%	—	—
Ripretinib	92.8%	—	—
Tivozanib	91.8%	—	—
Repotrectinib	87.1%	—	—
Cabozantinib	79.8%	—	—
Erdafitinib	78.9%	—	—
Crizotinib	78.1%	—	—
Brigatinib	75.0%	—	—
Pemigatinib	74.5%	—	—
Neratinib	73.9%	—	—
Selpercatinib	61.7%	—	—
Axitinib	56.9%	—	—
Infigratinib	56.2%	—	—
Nintedanib	54.7%	—	—
Vandetanib	51.4%	—	—
Defactinib	48.0%	—	—
Apatinib	37.5%	—	—
Pacritinib	37.4%	—	—
Umbralisib	35.8%	—	—
Entrectinib	30.1%	—	—
Canertinib	28.5%	—	—
Bosutinib	25.0%	—	—
Upadacitinib	22.0%	—	—
Futibatinib	20.7%	—	—
Regorafenib	17.9%	—	—

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