CCR4-351 是口服有效和选择性的CCR4拮抗剂。CCR4-351 具有新颖的哌啶基-氮杂环丁烷基序，在钙流量和 CTX 分析中的IC50为 22 nM 和 50 nM。CCR4-351 具有抗肿瘤活性。
| 生物活性 | CCR4-351 is an orally active, potent and selectiveCCR4antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, hasIC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | CCR4-351 (compound 38) shows no activity in a CYP450 induction assay[1].
CCR4-351 inhibits the migration of mouse iTregcells with an IC50of 39 nM, while the IC50in human iTregcells is 33 nM[1].
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体内研究
(In Vivo) | CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth[1].
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 T1/2of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse[1].
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[1].
| Animal Model: | Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor[1] | | Dosage: | 50 mg/kg | | Administration: | PO; daily; for 40 days | | Result: | Significantly reduced the tumor growth. |
| Animal Model: | Rat and mouse[1] | | 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 T1/2of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 190 mg/mL(379.68 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9983 mL | 9.9916 mL | 19.9832 mL | | 5 mM | 0.3997 mL | 1.9983 mL | 3.9966 mL | | 10 mM | 0.1998 mL | 0.9992 mL | 1.9983 mL |
*请根据半岛bd体育手机客户端
在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的半岛bd体育手机客户端
失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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