CCX-777 formic 

CCX-777 formic is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 formic induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 formic functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 formic is widely used in cancer-related research^[1][2][3][4].

CCX-777 formic (20 μM; 60 min) effectively prevents the reassociation of CXCL12^WT with ACKR3^WT in Sf9 cells, enabling quantitative analysis of the slow dissociation half-life (102 min) of CXCL12^WT from this receptor^[2].
CCX-777 formic (20 μM) specifically blocks the binding of CXCL12^WT to ACKR3^WT in Sf9 cells^[2].
CCX-777 formic (33 nM; 15 min) acts as a partial agonist for β-arrestin-2 recruitment to ACKR3 in HEK293S cells, with 52% efficacy relative to CXCL12 and a potency of ^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

639.81

C₃₂H₄₅N₇O₅S

Solid

Light green to green

O=C(NCCN1CCCC1)CC(N2CCN(C3=C4N=CC=CC4=CC=C3OC)CCC2)C5=CSC(N6CCOCC6)=N5.O=CO

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Santagata S, et al. CXCR4 and CXCR7 Signaling Pathways: A Focus on the Cross-Talk Between Cancer Cells and Tumor Microenvironment. Front Oncol. 2021;11:591386. Published 2021 Apr 15.  [Content Brief]

  [2]. Gustavsson M, et al. Kinetics of CXCL12 binding to atypical chemokine receptor 3 reveal a role for the receptor N terminus in chemokine binding[J]. Science signaling, 2019, 12(598): eaaw3657.

  [3]. Lounsbury N. Advances in CXCR7 modulators[J]. Pharmaceuticals, 2020, 13(2): 33.

  [4]. Gustavsson M, et al. Structural basis of ligand interaction with atypical chemokine receptor 3. Nat Commun. 2017;8:14135. Published 2017 Jan 18.  [Content Brief]