CCR4-351 hydrochloride 是口服有效和选择性的 CCR4 拮抗剂。CCR4-351 hydrochloride 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 hydrochloride 具有抗肿瘤活性。

CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity.

Solid

CCR4

CCR4-351 (compound 38) hydrochloride shows no activity in a CYP450 induction assay.
CCR4-351 hydrochloride inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

CCR4-351 (compound 38; 50 mg/kg; PO; daily; for 40 days) hydrochloride significantly reduces the tumor growth.
CCR4-351 (0.5 mg/kg; IV) hydrochloride 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 hydrochloride has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4-351 hydrochloride 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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 170 mg/mL (Need ultrasonic)In Vivo:请根据您的实验动物和给药