| Name | TL02-59 |
| Description | TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth. |
| In vitro | TL02-59 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. TL02-59 induces growth arrest in primary AML bone marrow samples. In TF-1 myeloid cells, TL02-59 (0.1, 1, 10, 100, 1000 nM; 6 h) potently inhibits Fgr autophosphorylation in TF-1 cells, with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range[1]. |
| In vivo | In mice, TL02-59 (1, 10 mg/kg; oral) completely eliminates AML cells from the spleen and peripheral blood while dramatically suppressing bone marrow involvement. TL02-59 has a t1/2 of 5.7 h by i.v and 6.5 h by p.o., respectively[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 120 mg/mL (196.84 mM), Sonication is recommended.
|
| Keywords | TL-02-59 | Inhibitor | Lyn | Apoptosis | leukemia | inhibit | acute | Src | orally | AML | TL02-59 | TL02 59 | TL0259 | Hck | myelogenous | Fgr |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Metabolism Compound Library | Inhibitor Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library |
United States
