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    AUNP-12
    AUNP-12

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V3096
    CAS #: 1353563-85-5Purity ≥98%

    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.


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    Molecular Weight (MW) 3261.55
    Formula C142H226N40O48
    CAS No. 1353563-85-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: N/A
    Water: ~100 mg/mL (30.6 mM)
    Ethanol: N/A
    AA sequenceSNTSESFK(SNTSESF-NH)FRVTQLAPKAQIKE-NH2
    Synonyms

    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-α-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-α-glutamine

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

    Exact Mass: 3259.6473 


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    In Vitro

    In vitro activity:  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. 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.


    Kinase Assay:   AUNP-12 displays an EC50 = 0.72 nM in the inhibition of binding PD1 to PD-L2 using hPDL2
    expressing HEK293 cells, and an EC50 = 0.41 nM in a rat peripheral blood mononuclear cells (PBMC) proliferation assay using hPDL1 expressing MDA-MB231 cells. This corresponds well to the ‘sub-nanomolar potency in disruption of PD1-PDL1/2 interaction’ reported for AUNP-012.


    Cell Assay: AUNP-12 displays an EC50 = 0.72 nM in the inhibition of binding PD1 to PD-L2 using hPDL2
    expressing HEK293 cells, and an EC50 = 0.41 nM in a rat peripheral blood mononuclear cells (PBMC) proliferation assay using hPDL1 expressing MDA-MB231 cells.

    In Vivo AUNP-12 inhibits by 44% tumor growth of B16F10 mouse melanoma cells injected subcutaneously in mice (5 mg/kg, subcutaneously once daily, 14 days); it reduces lung metastasis of B16F10 cells injected iv. in mice (5 mg/kg, subcutaneously, once daily, 11 days); it inhibits by 44% tumor growth of 4T1 cells injected orthotopically to mammary fat pad in mice (3 mg/kg, subcutaneously, once daily, 40 days). 10% of the animals treated with AUNP-12 showed complete regression and another 10% showed partial regression of tumor growth.  AUNP-12 treated animals showed a mean reduction in lung metastasis, measured after euthanasia, to the extent of >60%.
    Animal model Mouse with B16F10 melanoma tumor
    Formulation & Dosage
    References US Patent application US 2011/0318373, 29 Dec 2011; Cancer Research, vol. 72, no. 8 Suppl. 1, Abstract 2850, 2012.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    AUNP-126370779033200201486274341.pdf




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