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AUNP-12
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AUNP-12图片
CAS NO:1353563-85-5
规格:≥98%
包装与价格：
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
理化性质和储存条件
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[C@H](NC([C@@H](NC([C@@H](NC([C@H](CCC(N)=O)NC([C@H](C)NC([C@@H](NC([C@@H]1CCCN1C([C@H](C)NC([C@H](CC(C)C)NC([C@H](CCC(N)=O)NC([C@@]([C@H](O)C)([H])NC([C@H](C(C)C)NC([C@H](CCCNC(N)=N)NC([C@H](CC2=CC=CC=C2)NC([C@H](CCCCNC([C@H](CC3=CC=CC=C3)NC([C@@H](NC([C@H](CCC(O)=O)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)CO)=O)CC(N)=O)=O)[C@H](O)C)=O)CO)=O)=O)CO)=O)=O)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CO)NC([C@H]([C@H](O)C)NC([C@H](CC(N)=O)NC([C@@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)[C@@H](C)CC)=O)CCCCN)=O)C(N)=O)=O

Exact Mass: 3259.6473

实验参考方法
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.