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.
To enable antibody characterization methodsACROBiosystems has developed a series of enzymes.such as ldeS, SpeB, EndoH, and Endo S proteases, toassist with the characterization of antibodies and theirrelated post-translational modifications (PTMs)
ACROBiosystems developed a series of GMP grade cytokines under the GMP grade quality management system. Those products are all suitable for T/NK cell generation, activation, and proliferation in cell therapy research.
50+ targets designed for CAR detection, including PE/FITC/biotin labeled proteins. The key reagents for CD19 and BCMA were FDA DMF filed which can support your IND, NDA and BLA process.
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.
A series of immune checkpoints including classic co-inhibitory and co-stimulatory receptors. The comprehensive catalog contains 100+ targets with various species and tags, and the high-quality proteins are in good batch-to-batch consistency.
To meet the needs of ADCs development, ACROBiosystems can provide: A variety of high-quality target proteins; MMPs/Cathepsin/uPA for cleavable linker; Anti-payload antibodies & anti-idiotypic antibodies for immunogenicity and PK analysis; SPR/BLI analytical and ADA development service.
Comprehensive collection of Fc receptor proteins, including their common variants, which can help expedite your antibody development.
Comprehensive cytokine targets including interleukins, growth factors, chemokines, TNFs, etc. are expressed by HEK293 to ensure their natural structure. Their high purity is verified by SDS-PAGE/HPLC/SEC-MALS and high bioactivity is verified by ELISA/SPR/BLI.
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.
This web search service is supported by Google Inc.