Quinolines and derivatives
Medchemexpress LLC Apalutamide | 956104-40-8 | 99.9% | 477.43 | 200 MG
Apalutamide is a potent and competitive antagonist of the androgen receptor (AR), binding to it with an IC50 of 16 nM. It is intended for research use.
- Exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor, potentially antagonizing GABAA at therapeutic dose levels.
- Targets the AR ligand-binding domain, preventing AR nuclear translocation, DNA binding, and transcription of AR gene targets.
- Shows low systemic clearance, high oral bioavailability, and a long plasma half-life in both mouse and dog, supporting once-daily oral dosing.
- Achieves increased steady-state plasma levels in repeat-dose studies, resulting in high C24hr levels and low peak:trough ratios (2.5).
- Demonstrated significant tumor-volume reduction in castrate male mice bearing LNCaP/AR xenograft tumors.
Medchemexpress LLC Hypoxystat | 2414508-40-8 | 99.28% | 367.40 | 200 MG
Hypoxystat | 2414508-40-8 | 99.28% | 367.40 | 200 MG
eMolecules 3-AMINOISOQUINOLINE-8-CARBOXYLIC ACID HCL | 1337882-40-2 | MFCD28291832 | 1g
AstaTech | 3-AMINOISOQUINOLINE-8-CARBOXYLIC ACID HCL | 1g | 200614905 | 68507 | 95.000 | 1337882-40-2 | MFCD28291832 | 224.640 | C10H9ClN2O2
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Apexbio Technology LLC SCH 527123 473727-83-2 200mg
SCH 527123 (CAS 473727-83-2) is a selective antagonist of chemokine receptor 2 (CXCR2) It inhibits CXCR2-mediated signaling pathways by reducing phosphorylation events within the NF- B MAPK and AKT signaling cascades In colorectal cancer cell lines SCH 527123 suppresses cell growth in a dose-dependent manner with reported IC50 values ranging from approximately 18 to 40 mol/L after a 72-hour treatment Elevated IL-8 expression in cell lines such as HCT116 and Caco2 correlates with decreased sensitivity to SCH 527123 This compound is utilized in research investigating CXCR2 signaling in inflammation and tumor growth
Apexbio Technology LLC TAK-901 934541-31-8 200mg
TAK-901 (CAS 934541-31-8) is a small-molecule inhibitor primarily targeting Aurora B kinase with reported IC50 values of 0 0017 M for Aurora-B/INCENP and 0 021 M for Aurora-A/TPX2 Derived from an azacarboline kinase hinge-binding chemotype TAK-901 demonstrates time-dependent selective inhibition of Aurora B suppressing histone H3 phosphorylation and inducing polyploidy in vitro It inhibits proliferation across a range of human cancer cell lines (40 500 nM) and additionally targets kinases such as FLT3 and FGFR2 in cells In preclinical rodent xenograft models TAK-901 reduces tumor growth and induces complete regression in ovarian cancer models A phase I clinical trial has evaluated its dosing and pharmacokinetic characteristics in patients with advanced solid tumors and lymphomas