| Bioactivity | TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth[1]. |
| Invitro | TL02-59 dihydrochloride (0.1-1000 nM; 6 hours) 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]. TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency[1]. TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples[1]. Western Blot Analysis[1] Cell Line: |
| Name | TL02-59 dihydrochloride |
| CAS | 2415263-06-6 |
| Formula | C32H36Cl2F3N5O4 |
| Molar Mass | 682.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |