CTLA-4 inhibitor

Cas No.:	635324-72-0
Chemical Name:	MDK24720
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 - inhibitor;CTLA-4-inhibitor;BCP16856;AK499429;2-(4-fluorophenyl)-6-methyl-4-(3-(trifluoromethyl)phenyl)-1,6-dihydrodipyrazolo[3,4-b:3',4'-d]pyridin-3(2H)-one;4-{6-[(1E,2E)-2-(3-Methylbenzylidene)hydrazino]-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl}morpholine methanesulfona;B7/CD28 interaction inhibitor 1
SMILES:	FC(C1=C([H])C([H])=C([H])C(=C1[H])C1=C2C(N(C3C([H])=C([H])C(=C([H])C=3[H])F)N([H])C2=C2C([H])=NN(C([H])([H])[H])C2=N1)=O)(F)F
Formula:	C21H13F4N5O
M.Wt:	427.363
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	B7/CD28 interaction inhibitor 1 is a potent B7.1-CD28 interaction inhibitor with an IC50 of 50 nM[1].
Target:	IC50: 50 nM (B7.1-CD28 interaction)[1]
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 molecules on T cells with B7 molecules on antigen 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[1].
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.