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AZD0011

Chemical Structure : AZD0011

CAS No.: 2374807-41-5

AZD0011 (AZD-0011)

Catalog No.: PC-20187Not For Human Use, Lab Use Only.

AZD0011 (AZD-0011) a novel peptidic boronic acid prodrug of AZD0011-PL, highly potent and orally available Arginase (ARG) inhibitor with IC50 of 404/308 nM for ARG1/2, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

AZD0011 (AZD-0011) a novel peptidic boronic acid prodrug of AZD0011-PL, highly potent and orally available Arginase (ARG) inhibitor with IC50 of 404/308 nM for ARG1/2, respectively.
AZD0011 is the peptidic boronic acid prodrug ARG inhibitor payload (AZD0011-PL).
AZD0011 only inhibits extracellular ARG available in TME or periphery.
AZD0011 monotherapy leads to anti-tumor activity in multiple syngeneic tumor models.
AZD0011 shows combination benefit with an anti-NKG2A antibody in Balb/C mice bearing CT.26 WT tumors.
AZD0011 shows increased immune cell activation and anti-tumor activity when combined with anti-PD-L1 in MC38-OVA model.
AZD0011 potentiates type I IFN inducers anti-tumor efficacy.

Physicochemical Properties

M.Wt 329.20
Formula C14H28BN3O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(2R,4R)-4-((S)-2-amino-3-methylbutanamido)-2-(4-boronobutyl)pyrrolidine-2-carboxylic acid

References

1. Doshi AS, et al. Mol Cancer Ther. 2023 Mar 13:MCT-22-0431.

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