2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)- - Names and Identifiers
Name | KPT-276
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Synonyms | KPT276 KPT-276 CS-1100 KPT 276 (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one 2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)- (KPT276)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
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CAS | 1421919-75-6
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2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)- - Physico-chemical Properties
Molecular Formula | C16H10F8N4O
|
Molar Mass | 426.26 |
Density | 1.56±0.1 g/cm3(Predicted) |
Boling Point | 477.2±55.0 °C(Predicted) |
pKa | 0.59±0.50(Predicted) |
Storage Condition | -20℃ |
In vitro study | In MCL cells, KPT-276 resulted in significant growth inhibition and induction of apoptosis. KPT-276 specifically irreversibly inhibits the nuclear export function of XPO1 and reduces the activity of 12 HMCLs. In primary MM patient samples, KPT-276 were also effective in inducing apoptosis. |
In vivo study | In a xenograft AML mouse model, KPT-276 significantly prolonged survival and reduced leukemia burden in leukemic mice. In a severe combined immunodeficient mouse model with MCL, tumor growth was significantly inhibited by KPT-276 with no severe toxicities. In the Vk * MYC transgenic MM mouse model, KPT-276 reduced the spike of the monoclonal antibody, and in the xenograft MM mouse model, KPT-276 inhibited tumor growth. |
2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
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1 mM | 2.346 ml | 11.73 ml | 23.46 ml |
5 mM | 0.469 ml | 2.346 ml | 4.692 ml |
10 mM | 0.235 ml | 1.173 ml | 2.346 ml |
5 mM | 0.047 ml | 0.235 ml | 0.469 ml |
Last Update:2024-01-02 23:10:35
2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)- - Introduction
KPT-276 is a chemical and its full name is Selinexor. The following is a description of the nature, use, preparation and safety information of the KPT-276:
1. Nature:
- KPT-276 is a colorless crystalline solid, stable at room temperature.
-It is insoluble in water, but soluble in organic solvents such as dimethyl sulfoxide and acetone.
- KPT-276 has a higher melting point and lower volatility.
2. Use:
- KPT-276 is a selective nuclear transport inhibitor that can be used to treat some malignancies.
-It blocks the binding of the nuclear transporter XPO1 to the ribonucleic acid complex, thereby preventing the proliferation and spread of tumor cells.
- KPT-276 may be used to treat a variety of cancer types, including hematologic tumors such as multiple myeloma and lymphoma.
3. Preparation method:
-The method for preparing the KPT-276 includes an organic synthesis method and a crystallization purification method.
-Its synthetic route involves multiple steps of organic synthesis reaction and purification operation.
4. Safety Information:
-Strictly observe safety procedures when using the KPT-276, including wearing personal protective equipment such as gloves and goggles.
- KPT-276 may be toxic and harmful to humans and the environment, so be careful when using and handling.
-Avoid inhaling dusts or solutions and avoid direct contact with skin, eyes or esophagus when handling KPT-276.
-In case of accidental contact, rinse immediately with plenty of water and seek medical help.
-For detailed safety information and first aid measures on the KPT-276, consult the relevant safety data sheet before use.
Last Update:2024-04-09 20:49:11