Art. -Nr.: HY-112852

TL02-59

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

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.

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Reinheit: 99.86%
CAS. Nr.: 1315330-17-6
Formel: C₃₂H₃₄F₃N₅O₄
Molecular Weight:609.64

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

TL02-59 Chemical Structure

CAS. Nr.: 1315330-17-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Alle Src Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>10 μM Compound: 8	Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay	[PMID: 25075558]
BaF3	IC₅₀	0.092 μM Compound: 8	Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay	[PMID: 25075558]

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].

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

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 t_1/2 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-Prkdc^scidIl2rg^tm1Wjl/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.

Chemical Information

CAS. Nr. 1315330-17-6
Appearance Solid
Molecular Weight 609.64
Formel C₃₂H₃₄F₃N₅O₄
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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Journal Impact Factor

Cell Commun Signal

CD91-mediated reprogramming of DCs by immunogenic heat shock proteins requires the kinases AXL and Fgr. [Abstract]

2024 Dec 18;22(1):598. PMID: 39696592
Cell Death Discov

Inhibition of tyrosine kinase Fgr prevents radiation-induced pulmonary fibrosis (RIPF). [Abstract]

2023 Jul 17;9(1):252. PMID: 37460469
Cell Death Discov

Ionizing irradiation-induced Fgr in senescent cells mediates fibrosis. [Abstract]

2021 Nov 12;7(1):349. PMID: 34772919
J Transl Med

An Fgr kinase inhibitor attenuates sepsis-associated encephalopathy by ameliorating mitochondrial dysfunction, oxidative stress, and neuroinflammation via the SIRT1/PGC-1α signaling pathway. [Abstract]

2023 Jul 20;21(1):486. PMID: 37475042
Cell Rep

A positive feedback loop between FGR and p65 sustains satellite glial cell activation and chronic neuropathic pain. [Abstract]

2026 Jan 21;45(2):116899. PMID: 41575848
Neurosci Bull

Targeting Fgr-STAT3 Mediated Autophagy Inhibition in the Spinal Cord Alleviates Neuropathic Pain in Rats. [Abstract]

2026 Apr 9. PMID: 41957340
In Vivo

Silica Induced Lung Fibrosis Is Associated With Senescence, Fgr, and Recruitment of Bone Marrow Monocyte/Macrophages. [Abstract]

2021 Nov-Dec;35(6):3053-3066. PMID: 34697137
bioRxiv

2026 Feb 11.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (164.03 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Weir MC, et al. Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo. ACS Chem Biol. 2018 Jun 15;13(6):1551-1559. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6403 mL	8.2016 mL	16.4031 mL	41.0078 mL
	5 mM	0.3281 mL	1.6403 mL	3.2806 mL	8.2016 mL
	10 mM	0.1640 mL	0.8202 mL	1.6403 mL	4.1008 mL
	15 mM	0.1094 mL	0.5468 mL	1.0935 mL	2.7339 mL
	20 mM	0.0820 mL	0.4101 mL	0.8202 mL	2.0504 mL
	25 mM	0.0656 mL	0.3281 mL	0.6561 mL	1.6403 mL
	30 mM	0.0547 mL	0.2734 mL	0.5468 mL	1.3669 mL
	40 mM	0.0410 mL	0.2050 mL	0.4101 mL	1.0252 mL
	50 mM	0.0328 mL	0.1640 mL	0.3281 mL	0.8202 mL
	60 mM	0.0273 mL	0.1367 mL	0.2734 mL	0.6835 mL
	80 mM	0.0205 mL	0.1025 mL	0.2050 mL	0.5126 mL
	100 mM	0.0164 mL	0.0820 mL	0.1640 mL	0.4101 mL

Keywords

TL02-59

8 Cited Publications

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TL02-59

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) TL02-59

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TL02-59

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) TL02-59

Alle Src Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TL02-59 Related Classifications

HY-112852 Related Classifications