AUNP-12 - 半岛电竞官方网址

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 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

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 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 vitroactivity: 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.

In Vitro

In vitroactivity: 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.

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