AUNP-12

Description: AUNP-12 (also known as Aur-012, Aurigene-012, and Aurigene NP-12), a novel and potent immune checkpoint modulator developed by Aurigene Discovery Technologies, is an inhibitor of the PD-1 signalling pathway with an EC50 of 0.72 nM in the inhibition of binding PD1 to PD-L2 using hPDL2 expressing HEK293 cells, and an EC50 of 0.41 nM in a rat peripheral blood mononuclear cells (PBMC) proliferation assay using hPDL1 expressing MDA-MB231 cells. AUNP-12 is in development for the treatment of several cancers. It is the only peptide therapeutic in this pathway and may offer more effective and safer combination opportunities compared to current approaches such as antibodies including Nivolumab (BMS), Lambrolizumab (Merck-3475), CT-011 (Curetech), MDX-1105 (BMS), MPDL3280 (GNE) and MEDI-4736 (Medimmune-AZ), or Amplimmune’s PD-L2-FC fusion protein.

References: US 2011/0318373 A1; Yale Journal of Biology and Medicine, vol. 84, pp. 409-421, 2011; Cancer Research, vol. 72, no. 8 Suppl. 1, Abstract 2850, 2012.

Aurigene-012; Aur-012; Aurigene NP-12; Aurigene012; Aur012; Aurigene NP12; Aurigene 012; Aur 012; Aurigene NP 12

Chemical Name: N2, N6-bis(L-seryl-L-asparaginyl-L-threonyl-L-seryl-L-alpha-glutamyl-L-seryl-L-phenylalanyl)-L-lysyl-L-phenylalanyl-L-arginyl-L-valyl-L-threonyl-L-glutaminyl-L-leucyl-L-alanyl-L-prolyl-L-lysyl-L-alanyl-L-glutaminyl-L-isoleucyl-L-lysyl-L-alpha-glutamine

SMILES Code: OC(CC[CH](NC([CH](NC([CH](NC([CH](CCC(N)=O)NC([CH](C)NC([CH](NC([CH]1CCCN1C([CH](C)NC([CH](CC(C)C)NC([CH](CCC(N)=O)NC([C]([CH](O)C)([H])NC([CH](C(C)C)NC([CH](CCCNC(N)=N)NC([CH](CC2=CC=CC=C2)NC([CH](CCCCNC([CH](CC3=CC=CC=C3)NC([CH](NC([CH](CCC(O)=O)NC([CH](NC([CH](NC([CH](NC([CH](N)CO)=O)CC(N)=O)=O)[CH](O)C)=O)CO)=O)=O)CO)=O)=O)NC([CH](NC([CH](NC([CH](NC([CH](CO)NC([CH]([CH](O)C)NC([CH](CC(N)=O)NC([CH](N)CO)=O)=O)=O)=O)CCC(O)=O)=O)CO)=O)CC4=CC=CC=C4)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)CCCCN)=O)=O)=O)[CH](C)CC)=O)CCCCN)=O)C(N)=O)=O

Exact Mass: 3259.6473