MedKoo Cat#: 207209 | Name: SHR2554
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SHR2554, also known as EZH2-IN-15, is a potent EZH2 inhibitor that shows broad-spectrum anti-tumor efficacy in preclinical studies., SHR2554 inhibited proliferation and induced G1 phase arrest in EZH2-mutant DLBCL cell lines. The combination of EZH2 inhibitor SHR2554 with histone deacetylase (HDAC) inhibitor chidamide (hereafter referred to as HBI8000) exerted synergistic anti-proliferative activity in vitro and in vivo. Gene expression profile analysis revealed dramatic inhibition of the DNA replication process in combined treatment.

Chemical Structure

SHR2554
SHR2554
CAS#2098545-98-1

Theoretical Analysis

MedKoo Cat#: 207209

Name: SHR2554

CAS#: 2098545-98-1

Chemical Formula: C32H44N4O4

Exact Mass: 548.3363

Molecular Weight: 548.73

Elemental Analysis: C, 70.04; H, 8.08; N, 10.21; O, 11.66

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Synonym
SHR-2554; SHR 2554; SHR2554; EZH2-IN-15; zeprumetostatum; zeprumetostat
IUPAC/Chemical Name
N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-ethyl-6-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-(piperidin-1-ylmethyl)benzofuran-4-carboxamide
InChi Key
YLZVNQZYAYVUCW-UHFFFAOYSA-N
InChi Code
InChI=1S/C32H44N4O4/c1-5-25-28(36(6-2)23-10-14-39-15-11-23)18-29-26(17-24(40-29)20-35-12-8-7-9-13-35)30(25)32(38)33-19-27-21(3)16-22(4)34-31(27)37/h16-18,23H,5-15,19-20H2,1-4H3,(H,33,38)(H,34,37)
SMILES Code
O=C1NC(C)=CC(C)=C1CNC(C2=C3C=C(CN4CCCCC4)OC3=CC(N(C5CCOCC5)CC)=C2CC)=O
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Dysregulation of EZH2 has a crucial role in lymphomagenesis. We did a first-in-human study to assess the safety, pharmacokinetics, pharmacodynamics, and preliminary clinical activity of SHR2554, an oral EZH2 inhibitor, in patients with relapsed or refractory mature lymphoid neoplasms, including B-cell lymphomas, T-cell lymphomas, and classical Hodgkin lymphoma.

Preparing Stock Solutions

The following data is based on the product molecular weight 548.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Song Y, Jin Z, Li ZM, Liu Y, Li L, He C, Su H, Zhou H, Li K, Hao S, Zuo X, Wu J, Li D, Wu M, Sun X, Qi J, Cai Z, Li Z, Li Y, Huang Y, Shen J, Xiao Z, Zhu J. Enhancer of zeste homolog 2 inhibitor SHR2554 in relapsed or refractory peripheral T-cell lymphoma: data from the first-in-human phase 1 study. Clin Cancer Res. 2024 Jan 8. doi: 10.1158/1078-0432.CCR-23-2582. Epub ahead of print. PMID: 38190117. 2: Deng K, Zou Y, Zou C, Wang H, Xiang Y, Yang X, Yang S, Cui C, Yang G, Huang J. Study on pharmacokinetic interactions between SHR2554 and itraconazole in healthy subjects: A single-center, open-label phase I trial. Cancer Med. 2023 Jan;12(2):1431-1440. doi: 10.1002/cam4.5028. Epub 2022 Jul 16. PMID: 35841331; PMCID: PMC9883540. 3: Song Y, Liu Y, Li ZM, Li L, Su H, Jin Z, Zuo X, Wu J, Zhou H, Li K, He C, Zhou J, Qi J, Hao S, Cai Z, Li Y, Wang W, Zhang X, Zou J, Zhu J. SHR2554, an EZH2 inhibitor, in relapsed or refractory mature lymphoid neoplasms: a first-in- human, dose-escalation, dose-expansion, and clinical expansion phase 1 trial. Lancet Haematol. 2022 Jul;9(7):e493-e503. doi: 10.1016/S2352-3026(22)00134-X. PMID: 35772429. 4: Ryu YK, Amengual JE. Easy does it! New EZH2 inhibitor SHR2554 is safe and active in relapsed or refractory lymphoma. Lancet Haematol. 2022 Jul;9(7):e463-e465. doi: 10.1016/S2352-3026(22)00169-7. PMID: 35772421. 5: Wang X, Wang D, Ding N, Mi L, Yu H, Wu M, Feng F, Hu L, Zhang Y, Zhong C, Ye Y, Li J, Fang W, Shi Y, Deng L, Ying Z, Song Y, Zhu J. The Synergistic Anti- Tumor Activity of EZH2 Inhibitor SHR2554 and HDAC Inhibitor Chidamide through ORC1 Reduction of DNA Replication Process in Diffuse Large B Cell Lymphoma. Cancers (Basel). 2021 Aug 24;13(17):4249. doi: 10.3390/cancers13174249. PMID: 34503063; PMCID: PMC8428225.