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

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.

For research use only. We do not sell to patients.

AZD0011

AZD0011 Chemical Structure

CAS No. : 2374807-41-5

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Description

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)

In Vitro

AZD0011 potently inhibits recombinant Arg1 enzyme activity with an IC50 of 328 nM[1].

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

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 %
In Vivo

AZD0011 (3-100 mg/kg; p.o.; single dose) increases plasma and tumor arginine concentrations in Ag104Ld tumor bearing B6C3F1 mice[1].
AZD0011 (30 mg/kg; p.o.; twice daily; 17 days) produces significant tumor growth inhibition in Ag104Ld tumor-bearing mice[1].

MedChemExpress (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.
Molecular Weight

329.20

Formula

C14H28BN3O5

CAS No.
SMILES

OB(O)CCCC[C@@]1(C[C@H](CN1)NC([C@@H](N)C(C)C)=O)C(O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • 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.

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Product Name:
AZD0011
Cat. No.:
HY-182719
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