CCR4-351

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CCR4-351

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2174938-70-4

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

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]

CCR4

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 iT_regcells with an IC₅₀of 39 nM, while the IC₅₀in human iT_regcells is 33 nM^[1].

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 (V_ss=5.2 L/kg), a T_1/2of 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 (V_ss=5.2 L/kg), a T_1/2of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

分子量

500.42

性状

Solid

Formula

C₂₄H₂₇Cl₂N₇O

CAS 号

2174938-70-4

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

浓度溶剂体积质量

1 mg

5 mg

10 mg

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

请根据产品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产品失效。
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。