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

TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.

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TL02-59 dihydrochloride Chemical Structure

TL02-59 dihydrochloride Chemical Structure

CAS No. : 2415263-06-6

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TL02-59 dihydrochloride Related Antibodies

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Description

TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride 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 dihydrochloride (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 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency[1].
TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TL02-59 dihydrochloride Related Antibodies

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; 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

682.56

Formula

C32H36Cl2F3N5O4
CAS No.
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.Cl.Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TL02-59 dihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TL02-592415263-06-6SrcApoptosisorallyFgrLynHckacutemyelogenousleukemiaAMLInhibitorinhibitorinhibit

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