CCR4 antagonist 3

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CCR4 antagonist 3 

CCR4 antagonist 3 是口服有效和选择性的 CCR4 拮抗剂。CCR4 antagonist 3 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 antagonist 3 具有抗肿瘤活性。

CCR4 antagonist 3

CCR4 antagonist 3 Chemical Structure

CAS No. : 2174938-70-4

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CCR4 antagonist 3 的其他形式现货产品:

CCR4 antagonist 3 hydrochloride

生物活性

CCR4 antagonist 3 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].

IC50 & Target[1]

CCR4

 

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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].

Shanghai Jinpan Biotech Co Ltd 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[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 T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.

分子量

500.42

Formula

C24H27Cl2N7O
CAS 号

2174938-70-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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