CCR4-351|cas:2174938-70-4|西域试剂

CCR4-351,98.02%

产品编号：Bellancom-131349| CAS NO：2174938-70-4| 分子式：C₂₄H₂₇Cl₂N₇O| 分子量：500.42

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-131349		￥11500.00	杭州北京（现货）
Bellancom-131349		￥18000.00	杭州北京（现货）

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CCR4-351

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 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.

体外研究

CCR4-351 (compound 38) shows no activity in a CYP450 induction assay.
CCR4-351 inhibits the migration of mouse iT_reg cells with an IC₅₀ of 39 nM, while the IC₅₀ in human iT_reg cells is 33 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (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.

西域 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.

体内研究

西域 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.

性状

Solid

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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)

参考文献