NUCC-0226272

• CAT Number: I040072
• CAS Number: 3004503-12-9
• Molecular Formula: C67H91N9O8S
• Molecular Weight: 1182.56
• Purity: ≥95%
• Synonyms: (2S,4R)-1-[(2S)-2-[[11-[4-[[4-[3-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methylcarbamoyl]-5-[ethyl(oxan-4-yl)amino]-4-methylphenyl]phenyl]methyl]piperazin-1-yl]-11-oxoundecanoyl]amino]-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide
• InChI: InChI=1S/C67H91N9O8S/c1-9-75(53-27-33-84-34-28-53)57-37-52(36-55(46(57)4)63(80)69-40-56-44(2)35-45(3)71-64(56)81)50-23-21-49(22-24-50)41-73-29-31-74(32-30-73)60(79)18-16-14-12-10-11-13-15-17-59(78)72-62(67(6,7)8)66(83)76-42-54(77)38-58(76)65(82)68-39-48-19-25-51(26-20-48)61-47(5)70-43-85-61/h19-26,35-37,43,53-54,58,62,77H,9-18,27-34,38-42H2,1-8H3,(H,68,82)(H,69,80)(H,71,81)(H,72,78)/t54-,58+,62-/m1/s1
• InChIKey: GQULETMWOLCBGK-MUSRFAHESA-N
• SMILES: CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCN(CC5)C(=O)CCCCCCCCCC(=O)NC(C(=O)N6CC(CC6C(=O)NCC7=CC=C(C=C7)C8=C(N=CS8)C)O)C(C)(C)C

NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation. NUCC-0226272 has anti-proliferative effect. NUCC-0226272 has the potential for cancer research[1].
NUCC-0226272 (0.01-10 μM; 5 days) shows anti-proliferative effect in LNCaP and 22Rv1 cells[1].
NUCC-0226272 (10 μM; 6 days) shows strong degradation of EZH2, as well as reduction of PRC2 component SUZ12, and reduced H3K27me3 levels in C4-2B cells[1].
Pharmacokinetic Parameters of NUCC-0226272 in C57Bl/6 mouse[1].

IP (4 mg/kg)

Tmax (h)
0.83

Cmax (ng/mL)
3650

AUClast (min·ng/mL)
12777389

t1/2 (h)
3.46

CL (mL/min/kg)
3.11

Vss (L/kg)
3.11

Reference

[1]. Gary E. Schiltz, et al. Substituted 3-amino-5-phenylbenzamide compounds as covalent inhibitors of enhancer zeste homolog 2 (ezh2) and proteolysis-targeting chimeric derivatives thereof (protacs) that induce degradation of ezh2. US20230346953A1.