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CPI 360 is a selective EZH2 inhibitor with potent activity against both wild-type EZH2 and Y641N mutant EZH2. It effectively reduces cellular levels of H3K27me3 and H3K27me2, leading to cell cycle arrest and apoptosis in various non-Hodgkin’s lymphoma (NHL) cell lines. CPI 360 has demonstrated significant tumor growth reduction in preclinical studies, making it a promising therapeutic candidate for the treatment of NHL.

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  • 1802175-06-9 Structure
  • Basic information

    1. Product Name: CPI 360
    2. Synonyms: CPI 360;CPI360;CPI-360
    3. CAS NO:1802175-06-9
    4. Molecular Formula: C25H31N3O4
    5. Molecular Weight: 437.53134
    6. EINECS: N/A
    7. Product Categories: N/A
    8. Mol File: 1802175-06-9.mol
  • Chemical Properties

    1. Melting Point: N/A
    2. Boiling Point: 712.2±60.0 °C(Predicted)
    3. Flash Point: N/A
    4. Appearance: /
    5. Density: 1.26±0.1 g/cm3(Predicted)
    6. Refractive Index: N/A
    7. Storage Temp.: N/A
    8. Solubility: N/A
    9. PKA: 11.01±0.10(Predicted)
    10. CAS DataBase Reference: CPI 360(CAS DataBase Reference)
    11. NIST Chemistry Reference: CPI 360(1802175-06-9)
    12. EPA Substance Registry System: CPI 360(1802175-06-9)
  • Safety Data

    1. Hazard Codes: N/A
    2. Statements: N/A
    3. Safety Statements: N/A
    4. WGK Germany:
    5. RTECS:
    6. HazardClass: N/A
    7. PackingGroup: N/A
    8. Hazardous Substances Data: 1802175-06-9(Hazardous Substances Data)

1802175-06-9 Usage

Uses

Used in Oncology:
CPI 360 is used as a targeted therapy for the treatment of non-Hodgkin’s lymphoma (NHL). It works by inhibiting the EZH2 enzyme, which is overexpressed in various NHL cell lines, leading to a decrease in H3K27me3 and H3K27me2 levels. This inhibition triggers cell cycle arrest and apoptosis, effectively reducing tumor growth and potentially improving patient outcomes.
Used in Drug Development:
CPI 360 serves as a valuable compound in the development of novel therapeutic strategies for the treatment of non-Hodgkin’s lymphoma. Its selective inhibition of EZH2 and its demonstrated efficacy in preclinical studies make it a promising candidate for further research and development, potentially leading to the creation of new, more effective treatments for NHL patients.
Used in Preclinical Research:
CPI 360 is used as a research tool in preclinical studies to investigate the role of EZH2 in the development and progression of non-Hodgkin’s lymphoma. By studying the effects of CPI 360 on tumor growth and cell cycle regulation, researchers can gain a better understanding of the underlying mechanisms involved in NHL and identify potential targets for future therapeutic interventions.

Check Digit Verification of cas no

The CAS Registry Mumber 1802175-06-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,8,0,2,1,7 and 5 respectively; the second part has 2 digits, 0 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1802175-06:
(9*1)+(8*8)+(7*0)+(6*2)+(5*1)+(4*7)+(3*5)+(2*0)+(1*6)=139
139 % 10 = 9
So 1802175-06-9 is a valid CAS Registry Number.

1802175-06-9Downstream Products

1802175-06-9Relevant articles and documents

SUBSTITUTED BENZENE AND 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS

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, (2016/05/02)

The present invention relates to substituted benzene compounds and bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.

Discovery, design, and synthesis of indole-based EZH2 inhibitors

Gehling, Victor S.,Vaswani, Rishi G.,Nasveschuk, Christopher G.,Duplessis, Martin,Iyer, Priyadarshini,Balasubramanian, Srividya,Zhao, Feng,Good, Andrew C.,Campbell, Robert,Lee, Christina,Dakin, Les A.,Cook, Andrew S.,Gagnon, Alexandre,Harmange, Jean-Christophe,Audia, James E.,Cummings, Richard T.,Normant, Emmanuel,Trojer, Patrick,Albrecht, Brian K.

, p. 3644 - 3649 (2015/08/11)

The discovery and optimization of a series of small molecule EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit (2), a series of indole-based EZH2 inhibitors were identified. Biochemical potency and microsomal stability were optimized during these studies and afforded compound 22. This compound demonstrates nanomolar levels of biochemical potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

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Paragraph 0082; 0083, (2014/08/20)

Agents having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein.

MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF

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Paragraph 00308; 00309, (2013/08/28)

Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.

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