VZ185 - CAS 2306193-61-1

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VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively. VZ185 is a potent and selective VHL-based dual degrader of BRD7/9 (DC50 values are 4 and 34 nM for BRD7 and BRD9, respectively). Exhibits selectivity for BRD7/9 degradation over other bromodomain-containing proteins and other BAF/PBAF subunits. Displays cytotoxicity towards EOL-1 and A-204 cancer cell lines.

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Molecular Formula C53H67FN8O8S
Molecular Weight 995.21

VZ185

Synonyms VZ185; VZ-185; VZ 185; (2S,4R)-N-[[2-[5-[4-[[2,6-dimethoxy-4-(2-methyl-1-oxo-2,7-naphthyridin-4-yl)phenyl]methyl]piperazin-1-yl]pentoxy]-4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]-1-[(2S)-2-[(1-fluorocyclopropanecarbonyl)amino]-3,3-dimethylbutanoyl]-4-hydroxypyrrolidine-2-carboxamide
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 ZAGCLFXBHOXXEN-JPTLTNPLSA-N
InChI InChI=1S/C53H67FN8O8S/c1-33-46(71-32-57-33)34-11-12-35(27-56-48(64)42-26-37(63)29-62(42)50(66)47(52(2,3)4)58-51(67)53(54)14-15-53)43(23-34)70-22-10-8-9-17-60-18-20-61(21-19-60)31-41-44(68-6)24-36(25-45(41)69-7)40-30-59(5)49(65)39-28-55-16-13-38(39)40/h11-13,16,23-25,28,30,32,37,42,47,63H,8-10,14-15,17-22,26-27,29,31H2,1-7H3,(H,56,64)(H,58,67)/t37-,42+,47-/m1/s1
Canonical SMILES CC1=C(SC=N1)C2=CC(=C(C=C2)CNC(=O)C3CC(CN3C(=O)C(C(C)(C)C)NC(=O)C4(CC4)F)O)OCCCCCN5CCN(CC5)CC6=C(C=C(C=C6OC)C7=CN(C(=O)C8=C7C=CN=C8)C)OC

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