AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist, which can inhibit the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3. The corresponding IC50 values are 8.0 nM and 8.2 nM respectively.

 

Brand: BCM

 

Target: CXCR

 

Signaling Pathways: Autophagy; GPCR/G Protein; Immunology/Inflammation

 

In Vitro: AMG487 is a small molecular weight antagonist of CXCR3. 66.1 tumor cells were pretreated with AMG487 prior to i.v. injection into immune-competent female mice. Antagonism of CXCR3 on 66.1 tumor cells inhibited experimental lung metastasis, and this antimetastatic activity was compromised in mice depleted of natural killer cells. Systemic administration of AMG487 also inhibited experimental lung metastasis. In contrast to the antimetastatic effect of AMG487, local growth of 66.1 mammary tumors was not affected by receptor antagonism. Murine mammary tumor cells express CXCR3 which facilitates the development of lung metastases.Indicate for the first time that a small molecular weight antagonist of CXCR3 has the potential to inhibit tumor metastasis.

 

Melting Point: 161.2℃ (ethyl acetate heptane )

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CCOC1=CC=C(C=C1)N2C(=O)C3=C(N=CC=C3)N=C2[C@@H](C)N(CC4=CN=CC=C4)C(=O)CC5=CC=C(C=C5)OC(F)(F)F  

 

InChIKey: WQTKNBPCJKRYPA-OAQYLSRUSA-N  

 

InChI: InChI=1S/C32H28F3N5O4/c1-3-43-25-14-10-24(11-15-25)40-30(38-29-27(31(40)42)7-5-17-37-29)21(2)39(20-23-6-4-16-36-19-23)28(41)18-22-8-12-26(13-9-22)44-32(33,34)35/h4-17,19,21H,3,18,20H2,1-2H3/t21-/m1/s1

 

Attribute
[Chem Name]	N-[(1R)-1-[3-(4-ethoxyphenyl)-4-oxopyrido[2,3-d]pyrimidin-2-yl]ethyl]-N-(pyridin-3-ylmethyl)-2-[4-(trifluoromethoxy)phenyl]acetamide
[Synonym]	AMG 487; AMG-487
[CAS No.]	473719-41-4
[Formula]	C32H28F3N5O4
[Molecular]	603.59
[Form]	A crystalline solid
[Storage]	Keep in dark place. Sealed in dry. Store in freezer, under -20°C

Goods Tag