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Table 1 KIT mutation and its activated downstream in GIST cell lines

From: KIT mutations and expression: current knowledge and new insights for overcoming IM resistance in GIST

Cell lines

KIT mutations

Mutation downstream

TKI resistance and IC50 (nM)

IM SU RE

Ref

GIST-T1+

Exon 11: V570-Y578 (Hom)

MAPK pathway

PI3K pathway

Wnt pathway

Notch pathway

STAT3

S S S

16.54 15.00 110.00

[41,42,43,44,45,46]

GIST-882+

Exon 13: K642E (Hom)

MAPK pathway

PI3K pathway

STAT3

R S R

173.00 54.00 503.00

[19, 40, 44, 47, 48]

GIST-48+

Exon 11: V560D (Hom)

Exon 17: D820A (Het)

MAPK pathway

PI3K pathway

JAK/STAT pathway

R R R

413.00 587.00 164.00

[44, 47, 49, 50]

GIST-430+

Exon 11: (V560-L576) (Het)

Exon 13: V654A (Het)

MAPK pathway

PI3K pathway

R R R

61.00 68.00 191.00

[44, 49,50,51]

GIST-BOE+

Exon 9: A502_Y503dup

MAPK pathway

R NR NR

NR

[52, 53]

GIST-PSW+

Exon 11: K558_G565delinsR

MAPK pathway

S NR NR

NR

[52, 54]

HG129+

Exon 11: 45 bp insertion between F591- 592G

MAPK pathway

S NR NR

42.00 NR NR

[55]

GIST-522−

Exon 11: delEVQWK554-558 (het)

NR

R NR NR

NR

[49]

GIST-62−

Exon 11: MYEVQWK552-558T (het)

NR

R NR NR

NR

[49]

GIST-226−

Exon 11: P551-W557 (Hom)

Exon 17: Y823D (Hom)

MAPK pathway

R R R

 > 5000.00 3856.00 > 5000.00

[44, 56]

GIST-48B−

Exon 11: V560D (Hom)

Exon 17: D820A (Het)

MAPK pathway

R R R

 > 5000.00 > 5000.00 > 5000.00

[44, 57]

GIST-5−

Exon 11

NR

NR

NR

[58]

GIST-474−

Exon 11

NR

NR

NR

[58]

HG209−

Exon 11: delYIDPTQL 570–576

Exon 17: D816H

MAPK pathway

R R NR

 > 1000.00 NR NR

[59]

GIST-544−

Exon9: AY503-504ins (Het)

MAPK pathway

STAT1 and STAT3

NR

NR

[60]

  1. IM Imatinib, SU Sunitinib, RE Regorafenib, Hom Homozygous, Het Heterozygous, + KIT positive,—KIT negative, S Sensitive, R Resistance, NR Not reported