General description
A cell-permeable quinazoline compound that acts as a potent and reversible CXCR4 antagonist (IC50 = 36.2 nM for SDF-1/CXCL12 binding to hCXCR4-transfected HEK293 membrane) with selectivity over closely related human chemokine receptors CXCR2, CCR2, CCR4 and CCR5 (IC50 >10 µM). Shown to inhibit CXCL12-induced Ca2+-mobilization and cell migration in hCXCR4-HEK293 cells (IC50 = 100.1 and 41 nM, respectively), and rapidly mobilize CXCR4+, CD34+ and CD133+ stem cells from bone marrow in C57BL/6 male mice (6 mg/kg, s.c).
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Wu, C.H., et al. 2012. Chem. Med. Chem.7, In press.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 574.63. Empirical Formula: C30H43N7 · 2HCl. Quality Level: 100. Assay: ≥. 98% (HPLC). form: solid. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. color: white. solubility: DMSO: 25 . mg/mL, water: 25 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: C1(N: C(NCC2: CC: C(CNCCCNC3CCCCC3)C: C2)N: C4NC5CCNCC5): C4C: CC: C1. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51111840
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 239822-10MG