(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-
CPI-203
CAS: 1446144-04-2
Molecular Formula: C19H18ClN5OS
(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin- - Names and Identifiers
(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin- - Physico-chemical Properties
| Molecular Formula | C19H18ClN5OS |
| Molar Mass | 399.9 |
| Density | 1.51±0.1 g/cm3(Predicted) |
| Boling Point | 690.4±65.0 °C(Predicted) |
| Appearance | powder |
| Color | white to beige |
| pKa | 16.00±0.40(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | CPI203 inhibits BRD4 in vitro and in cells without affecting BRD4 kinase activity in vitro. CPI203 showed cell growth inhibition in all 9 MCL cell lines with GI50 ranging from 0.06 to 0.71 μm and low toxicity in normal PBMCs of healthy volunteers. In addition, lenalidomide and CPI203, targeting IRF4 and MYC, effectively activate the cell death program of bortezomib-resistant MCL cells. CPI203 inhibits BRD4 in vitro and in cells without affecting BRD4 kinase activity in vitro. CPI203 showed cell growth inhibition in all 9 MCL cell lines with GI50 ranging from 0.06 to 0.71 μm and low toxicity in normal PBMCs of healthy volunteers. In addition, lenalidomide and CPI203, targeting IRF4 and MYC, effectively activate the cell death program of bortezomib-resistant MCL cells. |
| In vivo study | BRD4 regulates the phosphorylation of CTD Ser2 in vivo. In REC-1 tumor-bearing mice, lenalidomide combined with CPI203 (2.5 mg/kg, I. P.) abolished the expression of MYC and IRF4 and induced apoptosis, synergistically increases the anti-tumor effect of the individual agents. BRD4 regulates the phosphorylation of CTD Ser2 in vivo. In REC-1 tumor-bearing mice, lenalidomide combined with CPI203 (2.5 mg/kg, I. P.) abolished the expression of MYC and IRF4 and induced apoptosis, synergistically increases the anti-tumor effect of the individual agents. |
(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.501 ml | 12.503 ml | 25.006 ml |
| 5 mM | 0.5 ml | 2.501 ml | 5.001 ml |
| 10 mM | 0.25 ml | 1.25 ml | 2.501 ml |
| 5 mM | 0.05 ml | 0.25 ml | 0.5 ml |
Last Update：2024-01-02 23:10:35
(S)-2-(4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin- - Introduction
CPI-203 (also known as JQEZ5) is a chemical that belongs to the class of Schiff enzyme (SET7) inhibitors. It has a range of specific properties and uses.
CPI-203 is a white odorless solid, can also be a yellow powder. Its chemical formula is C26H27Cl2N3O4S, and the relative molecular mass is 558.47. Its structure contains a pyridoxone ring and a benzene ring, and is substituted with two chlorine atoms and a sulfonyl group. It has good solubility and can be dissolved in common organic solvents.
CPI-203 is mainly used in medical research, as a SET7 enzyme inhibitor, can regulate chromatin modification, thereby affecting cell gene expression. This drug is widely used in cancer research, stem cell therapy and immunotherapy.
There are various methods for preparing CPI-203, and organic synthetic chemical reactions are usually used. Among them, a common synthesis method is based on 2-chloro-4-nitrobenzene as the starting material, through a series of reaction steps, such as Nitro reduction, N-alkylation and hydrazide condensation, final synthetic CPI-203.
When using the CPI-203, you need to pay attention to its safety information. This compound has a certain risk, may cause irritation and damage to the human body, should follow the relevant safety procedures. During storage and handling, it is necessary to avoid contact with oxidants and acids, and at the same time pay attention to prevent the generation of dust and vapor to avoid inhalation or skin contact. If discomfort or accidental contact occurs, seek medical advice immediately.
CPI-203 is a white odorless solid, can also be a yellow powder. Its chemical formula is C26H27Cl2N3O4S, and the relative molecular mass is 558.47. Its structure contains a pyridoxone ring and a benzene ring, and is substituted with two chlorine atoms and a sulfonyl group. It has good solubility and can be dissolved in common organic solvents.
CPI-203 is mainly used in medical research, as a SET7 enzyme inhibitor, can regulate chromatin modification, thereby affecting cell gene expression. This drug is widely used in cancer research, stem cell therapy and immunotherapy.
There are various methods for preparing CPI-203, and organic synthetic chemical reactions are usually used. Among them, a common synthesis method is based on 2-chloro-4-nitrobenzene as the starting material, through a series of reaction steps, such as Nitro reduction, N-alkylation and hydrazide condensation, final synthetic CPI-203.
When using the CPI-203, you need to pay attention to its safety information. This compound has a certain risk, may cause irritation and damage to the human body, should follow the relevant safety procedures. During storage and handling, it is necessary to avoid contact with oxidants and acids, and at the same time pay attention to prevent the generation of dust and vapor to avoid inhalation or skin contact. If discomfort or accidental contact occurs, seek medical advice immediately.
Last Update：2024-04-09 19:05:02
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Product Name: CPI-203 Visit Supplier Webpage Request for quotation
CAS: 1446144-04-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1446144-04-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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