PROTAC B-Raf degrader 1

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PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf. With anti-cancer activity. PROTAC B-Raf degrader 2 is a PROTAC targeting on B-Raf, consist of B-Raf ligand RGS linked to CRBN ligand Pomalidomide. PROTAC B-Raf degrader 2 led to a significant degradation of B-Raf at concentration of both 5μM and 10μM in MCF-7 cells post 24h, accompanied with a downregulation of its downstream Mcl-1.

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Molecular Formula C36H37N5O12S
Molecular Weight 763.77
Synonyms N-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]-2-oxoethyl]-2-[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]anilino]acetamide
Solubility 10 mM in DMSO
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping Room temperature in continental US; may vary elsewhere
InChI Key AMOFJSISJOOLNX-OUKQBFOZSA-N
InChI InChI=1S/C36H37N5O12S/c1-50-21-15-28(52-3)22(29(16-21)53-4)12-13-54(48,49)19-20-8-10-27(51-2)25(14-20)37-17-31(43)38-18-32(44)39-24-7-5-6-23-33(24)36(47)41(35(23)46)26-9-11-30(42)40-34(26)45/h5-8,10,12-16,26,37H,9,11,17-19H2,1-4H3,(H,38,43)(H,39,44)(H,40,42,45)/b13-12+
Canonical SMILES COC1=C(C=C(C=C1)CS(=O)(=O)C=CC2=C(C=C(C=C2OC)OC)OC)NCC(=O)NCC(=O)NC3=CC=CC4=C3C(=O)N(C4=O)C5CCC(=O)NC5=O

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