c-Kit (V654A)

KIT · Variant type: point · HGVS: p.V654A

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Dasatinib	97.4%	2.6%	87.97
2	Nintedanib	97.4%	2.6%	90.23
3	Axitinib	97.2%	2.8%	93.23
4	Sunitinib	97.1%	2.9%	91.73
5	Tivozanib	95.8%	4.2%	92.42
6	Ponatinib	93.4%	6.6%	78.23
7	Pacritinib	92.0%	8.0%	88.64
8	Cabozantinib	89.9%	10.1%	92.73
9	Quizartinib	87.7%	12.3%	99.50
10	Ripretinib	82.3%	17.7%	92.95
11	Avapritinib	81.3%	18.7%	97.73
12	Bosutinib	80.5%	19.5%	87.22
13	Pexidartinib	79.4%	20.6%	99.49
14	Lenvatinib	79.3%	20.7%	97.74
15	Pazopanib	77.8%	22.2%	97.49
16	Apatinib	71.4%	28.6%	97.73
17	Sorafenib	52.1%	47.9%	96.72
18	Selpercatinib	43.1%	56.9%	96.72
19	Gilteritinib	41.4%	58.6%	88.97
20	Regorafenib	40.2%	59.8%	95.99
21	Pralsetinib	38.3%	61.8%	93.43
22	Imatinib	38.2%	61.8%	99.00
23	Repotrectinib	35.7%	64.3%	84.21
24	Vemurafenib	32.0%	68.0%	96.49
25	Defactinib	26.3%	73.7%	92.68

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)
Dasatinib	97.4%	—	—
Nintedanib	97.4%	—	—
Axitinib	97.2%	—	—
Sunitinib	97.1%	—	—
Tivozanib	95.8%	—	—
Ponatinib	93.4%	—	—
Pacritinib	92.0%	—	—
Cabozantinib	89.9%	—	—
Quizartinib	87.7%	—	—
Ripretinib	82.3%	—	—
Avapritinib	81.3%	—	—
Bosutinib	80.5%	—	—
Pexidartinib	79.4%	—	—
Lenvatinib	79.3%	—	—
Pazopanib	77.8%	—	—
Apatinib	71.4%	—	—
Sorafenib	52.1%	—	—
Selpercatinib	43.1%	—	—
Gilteritinib	41.4%	—	—
Regorafenib	40.2%	—	—
Pralsetinib	38.3%	—	—
Imatinib	38.2%	—	—
Repotrectinib	35.7%	—	—
Vemurafenib	32.0%	—	—
Defactinib	26.3%	—	—

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