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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $65 | In Stock | |
5 mg | $137 | In Stock | |
10 mg | $223 | In Stock | |
25 mg | $377 | In Stock | |
50 mg | $538 | In Stock | |
100 mg | $732 | In Stock | |
200 mg | $986 | In Stock | |
1 mL x 10 mM (in DMSO) | $178 | In Stock |
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. |
Targets&IC50 | Lyn:0.1 nM , FGR:0.03 nM , Hck:160 nM |
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]. |
Molecular Weight | 609.64 |
Formula | C32H34F3N5O4 |
Cas No. | 1315330-17-6 |
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. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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