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| | 2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one Basic information |
| Product Name: | 2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one | | Synonyms: | CTLA-4 - INHIBITOR;2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one;CTLA-4 - INHIBITO;MDK24720;B7/CD28 interaction inhibitor 1;Dipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one, 2-(4-fluorophenyl)-1,6-dihydro-6-methyl-4-[3-(trifluoromethyl)phenyl]-;2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b;CTLA-4 inhibitor 1 | | CAS: | 635324-72-0 | | MF: | C21H13F4N5O | | MW: | 427.35 | | EINECS: | | | Product Categories: | | | Mol File: | 635324-72-0.mol | ![2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one Structure](CAS/20180702/GIF/635324-72-0.gif) |
| | 2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one Chemical Properties |
| Boiling point | 599.5±60.0 °C(Predicted) | | density | 1.54±0.1 g/cm3(Predicted) | | storage temp. | Sealed in dry,Room Temperature | | solubility | DMSO: Soluble: =10 mg/ml | | form | Solid | | pka | 5.76±0.20(Predicted) | | color | Off-white to light yellow |
| | 2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one Usage And Synthesis |
| Uses | B7/CD28 interaction inhibitor 1 (copmound 6b) is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM[1]. | | Biological Activity | MDK 24720 (CTLA-4 inhibitor, copmound 6b) is a Cytotoxic T-Lymphocyte-Associated protein 4 (CTLA-4, CD152) inhibitor with IC50 of 50 nM for B7.1–CD28 inhibition. | | in vitro | Bivalent CTLA4 homodimers bridge bivalent B7.1 homodimers to form an unusually stable signaling complex. Blocking B7/CD28 interactions with monoclonal antibodies or soluble receptors results in immunosuppression and enhanced allograft survival, while B7/CTLA-4 blockade results in enhanced antitumor immune responses. The interaction of co-stimulatory antigen molecules on T cells with B7 molecules on presenting cells plays an important role in the activation of naive T cells. Consequently, agents that disrupt these interactions should have applications in treatment of transplant rejection as well as autoimmune diseases. | | target | | Target | Value | CD152
() | | B7.1–CD28
(Cell-free assay) | 50 nM |
| | References | [1] Green NJ, et al. Structure-activity studies of a series of dipyrazolo[3,4-b:3',4'-d]pyridin-3-ones binding to the immune regulatory protein B7.1. Bioorg Med Chem. 2003 Jul 3;11(13):2991-3013. DOI:10.1016/s0968-0896(03)00183-4 |
| | 2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one Preparation Products And Raw materials |
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