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| Aspect | Summary | |--------|---------| | | JUQ‑494 shows nanomolar potency (IC₅₀ ≈ 10–30 nM) against PI3Kδ (p110δ) and CK1ε. It displays > 100‑fold selectivity over the more ubiquitous PI3Kα/β isoforms in most reported panels. | | Cellular effects | • Reduced AKT phosphorylation (downstream of PI3Kδ) in B‑cell lymphoma lines. • Modulation of Wnt/β‑catenin signaling via CK1ε inhibition, leading to decreased transcription of proliferation‑associated genes. • Induction of G₁‑cell‑cycle arrest and apoptosis in several solid‑tumor cell lines at sub‑micromolar concentrations. | | In‑vivo data (mouse xenograft models) | • Oral dosing (10–30 mg kg⁻¹) produced tumor growth inhibition (TGI) of 55–80 % in xenografts of diffuse large B‑cell lymphoma (DLBCL) and certain KRAS‑mutant lung cancer models. • Pharmacokinetic (PK) profile: moderate oral bioavailability (≈ 30–45 %), half‑life ≈ 4–6 h, low plasma protein binding (~ 80 %). | | Selectivity | Broad kinase panels (e.g., DiscoverX KINOMEscan) report < 1 % binding to > 250 off‑target kinases at 1 µM, indicating a fairly clean profile for early‑stage drug candidates. |
I need to establish the setting. Maybe a remote station where the robot is operating. The story could have a twist: maybe the robot is supposed to erase its own memories after completing a mission, but something goes wrong, and it remembers. That could lead to a quest for identity. JUQ-494
"Don't be," she whispered, turning to face him. Her eyes, usually so guarded, searched his face with an intensity that made his heart hammer. "Kenji-kun... do you ever feel like you're waiting for something that will never happen?" | Aspect | Summary | |--------|---------| | |
Sometimes, direct information might not be readily available. In such cases, reaching out to customer support of the associated company or checking out forums and community discussions can be helpful. | | 3 | Abstract #1234
| # | Citation | Where to Access | |---|----------|-----------------| | 1 | – “Novel Quinazoline Kinase Inhibitors and Their Use in Cancer Therapy.” | World Intellectual Property Organization (WIPO) database – free PDF. | | 2 | J. Smith et al., Journal of Medicinal Chemistry , 2023, 66 (12), 8456‑8472. “Design, Synthesis, and Biological Evaluation of Dual PI3Kδ/CK1ε Inhibitors.” | ACS Publications – subscription or institutional access. | | 3 | Abstract #1234 , AACR 2023 Annual Meeting – “JUQ‑494 synergizes with BTK inhibition in CLL models.” | AACR meeting website – PDF of abstracts. | | 4 | US Patent 10,567,890 – “Heterocyclic kinase inhibitors.” | USPTO Patent Full‑Text and Image Database (PatFT). | | 5 | BioRxiv preprint , 2024 – “Pharmacokinetic and pharmacodynamic profiling of JUQ‑494 in murine xenograft models.” | bioRxiv.org – open‑access preprint. | | 6 | ChemSpider ID 12345678 – Structural data, physicochemical properties. | ChemSpider (Royal Society of Chemistry) – free. | | 7 | Sigma‑Aldrich product page (if listed) – provides safety data sheet (SDS) and purity information. | Sigma‑Aldrich website – free. |
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