2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. Arginase
  4. AZD0011

AZD0011 是 AZD0011-PL (HY-182718) 的前药，是一种具有口服活性的精氨酸酶 (arginase) 1 抑制剂，IC50 为 328 nM。AZD0011 可在体内水解并释放精氨酸酶抑制剂有效载荷，抑制精氨酸水解，提升血浆和肿瘤微环境中的精氨酸水平。AZD0011 可恢复固有免疫功能并抑制肿瘤生长。AZD0011 可用于癌症研究，例如纤维肉瘤。

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AZD0011

AZD0011 Chemical Structure

CAS No. : 2374807-41-5

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AZD0011 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AZD0011, a prodrug of AZD0011-PL (HY-182718), is an orally active arginase 1 inhibitor with an IC50 of 328 nM. AZD0011 undergoes in vivo hydrolysis to release an arginase inhibitor payload, inhibiting arginine hydrolysis, increases arginine levels in plasma and the tumor microenvironment. AZD0011 restores innate immune function and inhibits tumor growth. AZD0011 can be used for the research of cancer, such as fibrosarcoma[1].

IC50 & Target[1]

arginase 1

328 nM (IC50)

体外研究
(In Vitro)

AZD0011 可强效抑制重组 Arg1 酶活性，其 IC50 为 328 nM[1]。

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

AZD0011 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL AUC0-∞ AUC F
Rat[1] 2 mg/kg i.v. 33.3 mL/min/kg 3.1 μM·h / /
Rat[1] 5 mg/kg p.o. / / 0.24 μM·h 2.7 %
体内研究
(In Vivo)

AZD0011 (3-100 mg/kg；口服；单次给药) 可呈剂量依赖性升高携带 Ag104Ld 肿瘤的 B6C3F1 小鼠体内血浆和肿瘤中的精氨酸浓度[1]。
AZD0011 (30 mg/kg；口服；每日 2 次；连续 17 天) 可在荷 Ag104Ld 肿瘤小鼠中产生显著的肿瘤生长抑制作用[1]。

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

Animal Model: B6C3F1 (female, 5 weeks old, subcutaneous implantation of 1×106 Ag104Ld fibrosarcoma cells)[1]
Dosage: 30 mg/kg
Administration: p.o.; twice daily; 17 days
Result: Produced tumor growth inhibition .
Had a synergistic effect with anti-PDL1 antibody.
分子量

329.20

Formula

C14H28BN3O5
CAS 号
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.
纯度 & 产品资料
参考文献

AZD0011 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD00112374807-41-5AZD 0011AZD-0011Arginasefibrosarcomaarginase 1Arg1 enzymearginine hydrolysisAg104Ld tumortumor microenvironmentinnate immune functiontumor growthPepT1/2Inhibitorinhibitorinhibit

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产品名称：
AZD0011
目录号：
HY-182719
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