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Cat. No.: HY-182719

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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.

CAS No.: 2374807-41-5
Formula: C₁₄H₂₈BN₃O₅
Molecular Weight:329.20

Storage:

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

AZD0011 Chemical Structure

CAS No.: 2374807-41-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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	AUC_0-∞	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.

Chemical Information

CAS No. 2374807-41-5
Molecular Weight 329.20
Formula C₁₄H₂₈BN₃O₅
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Mlynarski SN, et al. Discovery of (2R,4R)-4-((S)-2-Amino-3-methylbutanamido)-2-(4-boronobutyl)pyrrolidine-2-carboxylic Acid (AZD0011), an Actively Transported Prodrug of a Potent Arginase Inhibitor to Treat Cancer. J Med Chem. 2024 Dec 12;67(23):20827-20841. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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