1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Src
    Apoptosis
  3. TL02-59

TL02-59 

Cat. No.: HY-112852 Purity: 99.52%
Handling Instructions

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 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 (AML) cell growth.

For research use only. We do not sell to patients.

TL02-59 Chemical Structure

TL02-59 Chemical Structure

CAS No. : 1315330-17-6

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Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
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50 mg USD 1650 In-stock
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100 mg USD 2250 In-stock
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Description

TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 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 (AML) cell growth[1].

IC50 & Target

IC50: 0.03 nM (Fgr), 0.1 nM (Lyn) and 160 nM (Hck)[1]

In Vitro

TL02-59 (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 inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency[1].
TL02-59 induces growth arrest in primary AML bone marrow samples[1].

Western Blot Analysis[1]

Cell Line: TF-1 myeloid cells
Concentration: 0.1, 1, 10, 100, 1000 nM
Incubation Time: 6 hours
Result: Inhibited Fgr autophosphorylation in TF-1 cells.
In Vivo

TL02-59 (oral administration; 1 and 10 mg/kg; for three weeks) completely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement[1].
TL02-59 has a t1/2 of 5.7 h by i.v injection and 6.5 h by p.o. administration, respectively[1].

Animal Model: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice with human MV4-11 AML cells[1]
Dosage: 1 and 10 mg/kg
Administration: Oral; for three weeks
Result: Eliminated AML cells from the spleen and peripheral blood in a mouse model of AML, while dramatically suppressing bone marrow involvement.
Molecular Weight

609.64

Formula

C₃₂H₃₄F₃N₅O₄

CAS No.

1315330-17-6

SMILES

O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(OC4=C5C=C(OC)C(OC)=CC5=NC=N4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (205.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6403 mL 8.2016 mL 16.4031 mL
5 mM 0.3281 mL 1.6403 mL 3.2806 mL
10 mM 0.1640 mL 0.8202 mL 1.6403 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.41 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

TL02-59SrcApoptosisorallyFgrLynHckacutemyelogenousleukemiaAMLInhibitorinhibitorinhibit

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TL02-59
Cat. No.:
HY-112852
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