| Description | K00135 (IMIDAZOPYRIDAZIN 1) is a selective inhibitor of Pim kinases and can be used in studies about gastric cancer and antileukemic therapeutics. |
| In vitro | K00135 dose-dependently impairs the survival of murine Ba/F3 cells that have been rendered cytokine independent by overexpression of human PIMs. K00135 impairs survival and clonogenic growth of a panel of human acute leukemia cells. Exposure of K00135 significantly suppresses in vitro growth of leukemic blasts from five acute myelogenous leukemia patients but not of normal umbilical cord blood mononuclear cells[3]. |
| Synonyms | K-00135, Imidazol[1,2-b]pyridazine 1, K 00135, IMIDAZOPYRIDAZIN 1 |
| molecular weight | 306.36 |
| Molecular formula | C18H18N4O |
| CAS | 869650-21-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 4.4 mg/mL (14.36 mM) |
| References | 1. Darby RA, et al. Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors. Cancer Chemother Pharmacol. 2015 Oct;76(4):853-64. 2. Yan B, et al. Clinical and therapeutic relevance of PIM1 kinase in gastric cancer. Gastric Cancer. 2012 Apr;15(2):188-97. 3. Pogacic V, et al. Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity. Cancer Res. 2007 Jul 15;67(14):6916-24. 4. Taparowsky EJ, Gerbi SA. Structure of 1.71 lb gm/cm(3) bovine satellite DNA: evolutionary relationship to satellite I. Nucleic Acids Res. 1982 Sep 25;10(18):5503-15. |