CCR4-351

CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity In Vitro CCR4-351 (compound 38) shows no activity in a CYP450 induction assay. CCR4-351 inhibits the migration of mouse iT reg cells with an IC 50 of 39 nM, while the IC 50 in human iT reg cells is 33 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth . CCR4-351 (0.5 mg/kg; IV) has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V ss =5.2 L/kg), a T 1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse . CCR4-351 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor Dosage: 50 mg/kg Administration: PO; daily; for 40 days Result: Significantly reduced the tumor growth. Animal Model: Rat and mouse Dosage: 0.5 mg/kg of IV; 2 mg/kg of PO Administration: IV or PO Result: Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat. Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (V ss =5.2 L/kg), a T 1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse. Form:Solid IC50& Target:CCR4

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