CAS NO: | 1353563-85-5 |
规格: | ≥98% |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Molecular Weight (MW) | 3261.55 |
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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 sequence | SNTSESFK(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 |
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 Cell Assay: AUNP-12 displays an EC50 = 0.72 nM in the inhibition of binding PD1 to PD-L2 using hPDL2 |
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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. |