PROTAC RET Degrader 2

PROTAC RET Degrader 2 (JW15) potently inhibits RET kinase in a cell-free biochemical assay with an IC₅₀ of 0.36 nM^[1].
PROTAC RET Degrader 2 (0.0762-500 nM; 0-240 h) potently degrades RET (DC₅₀ = 0.26 nM) and inhibits proliferation (GI₅₀ = 1.2 nM) in TT human medullary thyroid carcinoma cells, with near-complete RET depletion at 2-6 nM and complete degradation by 24 h at 10 nM^[1].
PROTAC RET Degrader 2 degrades RET (85.6% at 100 nM, DC₅₀ = 7.84 nM) and inhibits proliferation (GI₅₀ = 13.7 nM) in RET Ba/F3 cells^[1].
PROTAC RET Degrader 2 potently degrades RET (DC₅₀ = 8.77 nM) and inhibits proliferation (GI₅₀ = 15 nM) in TPC-1 human papillary thyroid carcinoma cells^[1].
PROTAC RET Degrader 2 potently degrades RET (DC₅₀ = 39.85 nM) and inhibits proliferation (GI₅₀ = 17 nM) in LC-2/ad human lung adenocarcinoma cells^[1].
PROTAC RET Degrader 2 (10 nM; 24 h) induced RET degradation in TT human medullary thyroid carcinoma cells is attenuated by pretreatment with selpercatinib or a CRBN binder, confirming it requires dual binding to RET and CRBN^[1].
PROTAC RET Degrader 2 (10 nM; 6 h) induces RET degradation in TT human medullary thyroid carcinoma cells via the ubiquitin-proteasome system, not autophagy^[1].
PROTAC RET Degrader 2 engages CRBN in BRD4-eGFP-mCherry HeLa cells, as demonstrated by dose-dependent rescue of dBET6-induced BRD4 degradation^[1].
PROTAC RET Degrader 2 (0.1-10 nM; 24 h) effectively inhibited RET phosphorylation and downstream signaling pathways (STAT3, ERK, S6RP) in human medullary thyroid carcinoma TT cells^[1].
PROTAC RET Degrader 2 (50 nM; 12 h) induces selective degradation of RET kinase at the kinome-wide level in RET Ba/F3 cells^[1].
PROTAC RET Degrader 2 (0.1-1 nM; 120 h) induces significant apoptosis in TT human medullary thyroid carcinoma cells at 1 nM after 120 h of treatment^[1].
PROTAC RET Degrader 2 (0.1-10 nM) potently inhibits 2D colony formation in TT human medullary thyroid carcinoma cells^[1].
PROTAC RET Degrader 2 (0.1-10 nM; 4 week) potently inhibits anchorage-independent 3D colony formation in TT human medullary thyroid carcinoma cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.