TL02-59

SKU: orb1308997

Description

TL02-59 is a potent and selective small-molecule inhibitor of the Src-family kinase Fgr (IC50 = 0.03 nM), with additional activity against Lyn and Hck. It demonstrates potent anti-proliferative effects in acute myelogenous leukemia (AML) cell cultures, supporting its use as a research tool for studying kinase signaling in hematological malignancies.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1315330-17-6
• MW: 609.64
• Purity: 98.77% (May vary between batches)
• Formula: C₃₂H₃₄F₃N₅O₄
• SMILES: CCN1CCN(Cc2ccc(NC(=O)c3ccc(C)c(Oc4ncnc5cc(OC)c(OC)cc45)c3)cc2C(F)(F)F)CC1
• Target: Hck,Src,Apoptosis
• Solubility: DMSO:120 mg/mL (196.84 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.56 mM)

Bioactivity

• Target IC50:
  FGR:0.03 nM |Hck:160 nM |Lyn:0.1 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

acute, AML, Apoptosis, c-Fgr, orally, Lyn, Inhibitor, inhibit, myelogenous, Fgr, leukemia, Hck, TL02 59, TL0259, TL-02-59, TL02-59, Src

Compound Identifiers

PubChem CID

71254350