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TL02-59 is a selective, orally active Src-family kinase Fgr inhibitor with IC50 of 0.03 nM, it also inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. 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 vivo, TL02-59 (1 and 10 mg/kg; oral; three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML.
| Molecular Weight | 609.64 |
| Formula | C32H34F3N5O4 |
| CAS Number | 1315330-17-6 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Src-bcr-Abl Products |
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Saracatinib (AZD0530) is an orally active small molecule Src inhibitor. |
| Bosutinib
Bosutinib (SKI-606) is a novel Bcr-Abl inhibitor with IC50 values of 0.1 to 0.3 umol/L. |
| Dasatinib
Dasatinib (BMS-354825) is a small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. |
| DCC-2036
DCC-2036 is an ABL inhibitor with IC50 of 0.8 and 2 nM for u-ABL1native and p-ABL1native, respectively. |
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