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BIOMARKER:

RET G810C

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Entrez ID:

Related biomarkers:

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KIF5B-RET fusion + RET G810C (3)

EGFR mutation + RET fusion (2)

KIF5B-RET fusion + RET G810S (2)

CCDC6-RET fusion + EGFR mutation (1)

CCDC6‐RET fusion + TERT promotor mutation (1)

GPRC6A-RET fusion + EGFR mutation (1)

KIF5B-RET fusion + EGFR exon 19 deletion (1)

KIF5B-RET fusion + MET amplification (1)

KIF5B-RET fusion + RET E732K (1)

KIF5B-RET fusion + RET L730I (1)

KIF5B-RET fusion + RET L730V (1)

KIF5B-RET fusion + RET M918T (1)

KIF5B-RET fusion + RET V804E (1)

KIF5B-RET fusion + RET V804M (1)

KIF5B-RET fusion + TP53 H193R + MYC amplification (1)

MET amplification + RET fusion (1)

PD-L1 overexpression + RET-CCDC6 fusion (1)

PD-L1 overexpression + RET-KIF5B fusion (1)

PD-L1 overexpression + RET-KIF5B fusion + TP53 mutation + AR mutation + RET rearrangement (1)

RET G810C + CCDC6-RET fusion (1)

RET amplification + TMB-H + PD-L1 expression (1)

RET positive + KRAS G12V (1)

RET positive + SMARCA4 mutation (1)

RET-MIR4299-MIR8070 fusion + RET amplification (1)

SHTN1-RET fusion + EGFR mutation (1)

SPECC1-RET fusion + EGFR mutation (1)

TLN1-RET fusion + EGFR mutation (1)

TRIM24-RET fusion + EGFR mutation (1)

TRIM33-RET fusion + EGFR mutation (1)

KIF5B-RET fusion + RET G810C (3)

EGFR mutation + RET fusion (2)

KIF5B-RET fusion + RET G810S (2)

CCDC6-RET fusion + EGFR mutation (1)

CCDC6‐RET fusion + TERT promotor mutation (1)

GPRC6A-RET fusion + EGFR mutation (1)

KIF5B-RET fusion + EGFR exon 19 deletion (1)

KIF5B-RET fusion + MET amplification (1)

KIF5B-RET fusion + RET E732K (1)

KIF5B-RET fusion + RET L730I (1)

KIF5B-RET fusion + RET L730V (1)

KIF5B-RET fusion + RET M918T (1)

KIF5B-RET fusion + RET V804E (1)

KIF5B-RET fusion + RET V804M (1)

KIF5B-RET fusion + TP53 H193R + MYC amplification (1)

MET amplification + RET fusion (1)

PD-L1 overexpression + RET-CCDC6 fusion (1)

PD-L1 overexpression + RET-KIF5B fusion (1)

PD-L1 overexpression + RET-KIF5B fusion + TP53 mutation + AR mutation + RET rearrangement (1)

RET G810C + CCDC6-RET fusion (1)

RET amplification + TMB-H + PD-L1 expression (1)

RET positive + KRAS G12V (1)

RET positive + SMARCA4 mutation (1)

RET-MIR4299-MIR8070 fusion + RET amplification (1)

SHTN1-RET fusion + EGFR mutation (1)

SPECC1-RET fusion + EGFR mutation (1)

TLN1-RET fusion + EGFR mutation (1)

TRIM24-RET fusion + EGFR mutation (1)

TRIM33-RET fusion + EGFR mutation (1)

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2ms

Discovery of 7-(1-methyl-1H-pyrazol-4-yl)-1,6-naphthyridine derivatives as potent inhibitors of rearranged during transfection (RET) and RET solvent-front mutants for overcoming selpercatinib resistance. (PubMed, Eur J Med Chem)

Importantly, 20p exhibited highly impressive antitumor potency in both a Ba/F3-KIF5B-RETWT-derived xenograft mouse model and a selpercatinib-resistant Ba/F3-KIF5B-RETG810R-positive mutant xenograft mouse model. Overall, 20p represents a novel and promising drug lead for overcoming RET solvent-front mutation-based resistance to selpercatinib.

2 months ago

Journal

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RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B)

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RET G810C • RET G810R • RET G810S

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Retevmo (selpercatinib)