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1. Clear MoA- Restores T Cell Function through Inhibition on Adenosine Signaling Pathway
(1) The asset treatment results in decrease of pCREB, a downstream PD marker of adenosine signaling.
(2) The asset antagonizes the immunosuppressive effects by NECA (adenosine analogue) and results in rescue of IL-2 and TNF-α secretion from CD4+ T cells and CD8+ T cells, which suggests the recovery of anti-tumor effects of T cells.
2. Shows Significant Monotherapy Activity
(1) The asset shows anti-tumor effects in a dose-dependent manner in the mouse MC38-hPD-L1 colorectal tumor model.
(2) The asset shows better anti-tumor activity than AB928 at the same dose.
(3) The asset reduces Treg infiltrated in tumors.
3. Significant Synergy with Tecentriq (PD-L1 mAb) &Keytruda (PD-1mAb)
(1) The asset has comparable anti-tumor effects with Tecentriq & Keytruda (PD-L1 mAb) in the mouse MC38-hPD-L1 colorectal tumor model/ humanized HCC827 NSCLC model.
(2) Combo of the asset and Tecentriq & Keytruda shows significant synergy.
4. Non-clinical TOX Studies were observed
(1) In the pivotal 4-week repeated dose toxicity with a 4-week recovery period in SD rats and beagle dogs, animals in this asset treated group were well tolerated, and a good safety margin (3.6 vs. NOAEL in dogs, 25.9 vs. HNSTD in rats) was achieved.
(2) The IC50 of hERG current was >40 μM.
(3) Showed low risk for the cardiovascular, respiratory and central nervous system in safety-pharmacology studies.
(4) No genotoxicity was noted in the chromosomal aberration test in Chinese hamster lung fibroblasts.
(5) No genotoxic effect on CD-1 mice bone marrow cells was observed in mice bone marrow micronucleus study.
1. Asset type: A2aR/A2bR Antagonist
2. Indication: Advanced/metastatic solid tumors or hematological malignancies
3. Research phase: IND approved (FDA)
4. Administration route oral Tablets(5 mg/25 mg/75 mg)
5. Cooperation demands: License-out (Ex-China) or co-development
6. Research progress:
(1) Project Advantages: The fourth A2aR/A2bR inhibitor worldwide, with the characteristics of high activity, high selectivity and low toxicity.
(2) Patent Strategy: The core patents are expected to be filed in major countries in October 2022. (CN, PCT, US, EP, JP, CA, AU, FR, SG etc.)
ACROBiosystems offers a wide selection of Matrigengel basement membrane extracts. Different versions – including phenol red-free, high concentration, iPSC culturing, organoid culturing – are all available for your specific needs to support 3D cell culture!
ComboX is a new brand of ACROBiosystems. ComboX products include our Streptavidin series products, coated plates, isotype controls for antibody and fusion protein drug research, and general-purpose antibodies.
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GMP grade cytokines, reagents for cell activation, gene edition, DNA/RNA removal, etc. Particularly focus on product design, quality control and solution-based support to link each phase of your cell and gene therapy journey.
Full length multi-pass TPs with stabilized structure and high bioactivity for immunization, antibody screening, cell based assay and CAR detection, including hot CD20, Claudin 18.2， CD133, GPRC5D，CCR8, CCR5, etc.
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Aneuro is ACROBiosystems brand focused on neuroscience research, providing high-quality important proteins including therapeutic and diagnostic research proteins, PFFs and recombinant neuro factors, etc. to advance neuroscience research.
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