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Tazemetostat HCl

CAT: 0931-T70588-01Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0931-T70588-01Size:25 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
1467052-84-1
Target
Others
Related Pathways
Others
Bioactivity
Tazemetostat HCl is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation. These data demonstrate the dependency of SMARCB1 mutant MRTs on EZH2 enzymatic activity and portend the utility of EZH2-targeted drugs for the treatment of these genetically defined cancers.
Smiles
Cl.CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)-c1ccc(CN2CCOCC2)cc1
Molecular Formula
C34H45ClN4O4
Molecular Weight
609.21
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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