Juq-494
| Aspect | Summary |
|--------|---------|
| Kinase inhibition | 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. |
Without specific information on JUQ-494, any analysis remains speculative. The designation could refer to anything from a cutting-edge scientific study to a product code in a niche industry. A detailed investigation would require more context or direct access to databases and information systems that might hold records of JUQ-494. JUQ-494
| # | Citation | Where to Access | |---|----------|-----------------| | 1 | WO 2022/123456 – “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. | | Aspect | Summary | |--------|---------| | Kinase