Compound 23

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化合物 23 选择性诱导 BRAF-V600E 降解，但不诱导野生型 BRAF 降解。

Compound 23 selectively induces degradation of BRAF-V600E but not wildtype BRAF.

PROTAC BRAF-V600E degrader-1 (compound 23) (1 nM-10 μM; 72 h) inhibits the cell viability of A375 and HT-29.PROTAC BRAF-V600E degrader-1 (1-1000 nM; 16 h or 0-24 h) inhibits p-ERK and BRAF-V600E protein in A375 cells. Cell Viability Assay Cell Line:A375 and HT-29 Concentration:1 nM-10 μM Incubation Time:72 h Result:Inhibited the cell viability of A375 and HT-29 with IC50s of 46.5 nM and 51 nM.Western Blot Analysis Cell Line:A375 Concentration:1, 4, 12, 37, 111, 333 and 1000 nM Incubation Time:16 h or 0-24 h Result:Induced the reduction in the phosphorylation of ERK.Inhibited p-ERK and BRAF-V600E in a dose- and time-dependent manner.

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MAPK/ERK Signaling

Raf

B-Raf (V600E)

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2417296-84-3

1001.07

C48H54F2N10O10S

>98% (HPLC)

DMSO:10 mM

CCCS(=O)(NC1=CC=C(F)C(N2C=C(C3=CN=CN=C3)C4=NC(N(C5CCN(C(CCOCCOCCOCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)CC5)C)=CC=C42)=C1F)=O

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(-20℃)

With Ice Pack

≥ 2 years