产品
编 号：F749654
分子式：C24H27Cl2N7O
分子量：500.42
分子式：C24H27Cl2N7O
分子量：500.42
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 2174938-70-4
产品详情
生物活性：
CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
体内研究：
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 (Vss=5.2 L/kg), a T1/2 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. 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 (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
体外研究：
CCR4-351 (compound 38) shows no activity in a CYP450 induction assay. CCR4-351 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM.
CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.
体内研究：
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 (Vss=5.2 L/kg), a T1/2 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. 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 (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
体外研究：
CCR4-351 (compound 38) shows no activity in a CYP450 induction assay. CCR4-351 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM.
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