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产地 | 中国 |
品牌 | Chemstan |
货号 | LC-01 |
用途 | 中间体 |
包装规格 | 20mg |
纯度 | 98%% |
CAS编号 | 1446144-04-2 |
是否进口 | 否 |
联合知名大学科研院所及企业开发药食两用植物标准品和天然植物有效单体,主打中药对照品/标准品/天然植物有效单体,小分子化合物库,药物杂质。所有产品仅用作科学研究,我们不为任何个人用途提供产品和服务。
Fields of Application :
CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).
CAS Number: | 1446144-04-2 |
Purity: | HPLC Purity>99%,ee purity>99% |
Molecular Weight: | 399.9 |
Molecular Formula: | C19H18ClN5OS |
Quality Control: HPLC、NMR、 LC/MS(Please contact us to get the QC report)
Synonyms: | CPI 203 |
Chemical Name: | |
Storage: | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
Note: Products for research use only, not for human use
Description:
CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay). It has an IC50 of ~99 nM in inhibiting Myc expression in MV4-11 cells and an IC50 of ~30 nM in inhibiting IL-6 production in THP-1 cells stimulated with LPS, decreases specific Ser2 phosphorylation of the carboxyl-terminal domain (CTD) of the RNA polymerase II (Pol II) by either endogenous BRD4 or a BRD4 mutant, BRD4 FEE-AAA, that is incapable of binding PTEFb. CPI203 is an analog of JQ-1 but has shown superior bioavailability with oral or intraperitoneal (IP) administration. When mice that were transplanted with primary mouse T-ALL cells, either Fbxw7+/+ or Fbxw7mut/+, were treated with CPI203 at 5 mg/Kg orally twice per day, a significant and rapid reduction in leukemia burden was observed. CPI203 is a useful chemical probe to study the suppression of Myc-dependent cancer development.For the detailed information of CPI203 (CPI-203), the solubility of CPI203 (CPI-203) in water, the solubility of CPI203 (CPI-203) in DMSO, the solubility of CPI203 (CPI-203) in PBS buffer, the animal experiment (test) of CPI203 (CPI-203), the cell expriment (test) of CPI203 (CPI-203), the in vivo, in vitro and clinical trial test of CPI203 (CPI-203), the EC50, IC50,and Affinity of CPI203 (CPI-203).
References:
CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)N)C4=CC=C(C=C4)Cl)C