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TL02-59

Cat. No. M9664
TL02-59 Structure
Synonym:

TL0259

Size Price Availability
5mg USD 350  USD350 4-7 Days
10mg USD 550  USD550 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 609.64
Formula C32H34F3N5O4
CAS Number 1315330-17-6
Purity >99%
Solubility DMSO ≥ 90 mg/mL
Storage at -20°C
References

[1] Mark C Weir, et al. ACS Chem Biol. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TL02-59, TL0259 supplier, Src-bcr-Abl, inhibitors

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