1. PI3Kδ selective inhibitor with a broad safety window
(1) As an important member of the PI3K/mTOR pathway which regulates cell proliferation and cell cycle, PI3Kδ is involved in early signaling responses of leukocytes in a wide variety of stimulations.
(2) PI3Kδ is only expressed in hematopoietic lineage, which remains a broad safety window for PI3Kδ selective inhibitors compared to pan-PI3K inhibitors or PI3Kα/β selective inhibitors.
(3) High expression of PI3Kδ is found in Hematologic malignancies patients.
2. A high selective inhibition of PI3Kδ in kinase and cellular level.
Asset against PI3Kδ increased by 16 times at kinase levels and by 2–14 times at cellular levels compared with Idelalisib.
3. Excellent anti-B cell activity and good safety in vivo.
(1) Inhibition of asset on rat-activated B cells were 4-fold (1 h) and 15-fold (8 h) higher than that of Idelalisib, respectively, with less toxic than Idelalisib at the same dose in a 28-day repeated-dose toxicity test in rats.
(2) hERG assay indicated the low risk of prolongation of QT interval and hERG block potency.
(3) No genotoxicity was observed in the preclinical toxicity study. No abnormality was observed in the cardiovascular and respiratory systems when administered in species of SD Rats and Beagle Dogs.
4. Clinical trial data: a suit for QD and a better AUC. (higher AUC than Idelalisib at a much lower dose)
(1) t1/2 = 16.4 h at a dose of 25 mg, which is suitable for QD.
(2) At the same dose, assets in humans showed a much higher AUC than Idelalisib.
1. Asset type: PI3Kδ inhibitor
2. Indication: Hematologic malignancies
3. Research phase: Phase I, China; the patent has been granted in the US
4. Cooperation demands: License-out or co-development
5. Research progress:
(1) High selective PI3Kδ inhibitor on phase 1 trial.
(2) No genotoxicity and no cardiovascular and respiratory system abnormality was observed in the pre-clinical study.
(3) Good AUC was shown in clinical trial.
Explore our catalog of therapeutic antibody solutions to find the right products for you! We are dedicated to delivering solutions designed to help you drive innovation and push the boundaries of what therapeutic antibodies can be.
Organoid Toolbox is a collection of organoid solutions including ready-to-use organoids, organoid differentiation kits, and a variety of services to accelerate the progress of your drug development project.
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 provides innovative solutions for neuroscience research. Recombinant proteins, neural factors, pre-formed fibrils, electrophysiological electrodes, as well as Organoid Toolbox all in Aneuro aiming to advance neuroscience research, develop therapeutic interventions, and improve diagnostic methods for neurological diseases.
This web search service is supported by Google Inc.