| Identification | Back Directory | [Name]
2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one | [CAS]
635324-72-0 | [Synonyms]
MDK24720
CTLA-4 - INHIBITO
CTLA-4 inhibitor 1
CTLA-4 - INHIBITOR
B7/CD28 interaction inhibitor 1
2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b
2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,2-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(6H)-one
Dipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one, 2-(4-fluorophenyl)-1,6-dihydro-6-methyl-4-[3-(trifluoromethyl)phenyl]- | [Molecular Formula]
C21H13F4N5O | [MDL Number]
MFCD28127008 | [MOL File]
635324-72-0.mol | [Molecular Weight]
427.35 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
| [storage]
Store at -20°C | [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 |
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