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CCR4 antagonist 3 hydrochloride
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。
CCR4 antagonist 3 hydrochloride图片
CAS NO:2174938-71-5
包装:5mg
市场价:10350元

产品介绍
CCR4 拮抗剂 3 hydrochloride 是一种具有口服活性、强效和选择性的 CCR4 拮抗剂。
Cas No.2174938-71-5
分子式C24H27Cl2N7O.xHCl
溶解度DMSO : 170 mg/mL (Need ultrasonic)
储存条件4°C, away from moisture
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].

CCR4 antagonist 3 (compound 38) shows no activity in a CYP450 induction assay[1].CCR4 antagonist 3 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM[1].

CCR4 antagonist 3 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth[1].CCR4 antagonist 3 (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[1].CCR4 antagonist 3 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4 antagonist 3 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].

[1]. Omar Robles, et al. Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as Single Agent and in Combination with Checkpoint Inhibitors. J Med Chem. 2020 Jul 15.