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Cat. No. Product Name CAS No. Information
PC-35514

AZ084

929300-19-6

AZ084 (AZ-084) is a potent, selective, allosteric, orally available CCR8 antagonist with Ki of 0.9 nM; demonstrates excellent selectivity in a panel of 141 kinases and receptors, also shows no binding activity at 10 uM towards any of the other chemokine receptors; demonstrates excellent selectivity, high metabolic stability in vitro and an attractive in vivo PK profile with a long half-life in rats; inhibits dendritic cell, T cell and eosinophil migration.

PC-61979

ML 604086

850330-18-6

ML 604086 (ML604086) is a potent, selective CCR8 inhibitor that inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations with IC50 of 1.3 uM and 1.0 uM respectively in cellular assays; displays high selectvity against a panel of 40 GPCRs, only moderately inhibits 5HT1a (30% at 10 uM).

PC-61687

AZD 2098

566203-88-1

AZD2098 is a potent, selective, orally bioavailable CCR4 receptor antagonist with pIC50 of 7.8 for hCCR4, pIC50 of 8.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.3; exhibits anti-inflammatory effects in Brown-Norway rats sensitized to ovalbumin.

Asthma

Phase 1 Clinical

PC-61576

INCB10820

1310796-72-5

INCB10820 (PF-4178903) is a potent, selective, orally bioavailable dual CCR2 and CCR5 antagonist with binding IC50 of 3.0 nM and 5.3 nM, respectively; displays an IC50 of 4.3 nM in CCR5 chemotaxis functional assay; is active against mouse, rat and cynomolgus monkey CCR2 with binding IC50 of 2.8, 2.9 and 4.6 nM, respectively, but inactive against canine CCR2, also is active against mouse and cynomolgus monkey CCR5 with IC50 of 71 and 4.0 nM, respectively.

PC-61557

PF-04136309

1341224-83-6

PF-4136309 (INCB8761) is a potent, selective, competitive, reversible full CCR2 antagonist with IC50 of 2-5 nM; depletes inflammatory monocytes and macrophages from the primary tumor and premetastatic liver resulting in enhanced antitumor immunity, decreased tumor growth, and reduced metastasis.

Pancreatic Cancer

Phase 2 Clinical

PC-61317

LY-2510924

1088715-84-7

LY-2510924 (LY2510924) is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM, without apparent agonist activity; inhibits SDF-1-induced cell migration with IC50 of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling; exhibits inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells; shows inhibition of tumor growth in human xenograft models with acceptable in vivo stability and a pharmacokinetic profile.

Kidney Cancer

Phase 2 Clinical

PC-60972

LMD-009

950195-51-4

LMD-009 (LMD 009, LMD009) is a potent, selective, nonpeptide CCR8 agonist that stimulates CCR8-mediated chemotaxis, inositol phosphate accumulation and calcium release with EC50 of 11-87 nM; displays no activity against other chemokine receptors.

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