| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
TL02-59 is a novel, potent and orally bioavailable Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 also inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
| ln Vitro |
TL02-59 (0.1-1000 nM; 6 hours) substantially reduces Fgr autophosphorylation in TF-1 cells, with moderate inhibition at 0.1-1 nM and total inhibition beyond 10 nM. Hck, Lyn and Flt3 are effective in regulating nM in the proliferation of TL02-59 primary AML cell lines and induce cell inhibition [1]. TL02-59 is suppressed in primary AML cell samples in the range of 100 to 1000 nM [1].
|
|---|---|
| ln Vivo |
AML cells in the spleen and peripheral blood were totally eradicated by TL02-59 (package insert; 1 mg/kg and 10 mg/kg; for three weeks) while cell involvement in the AML model was markedly inhibited [1]. For intravenous and intravenous hour formulations, the t1/2 of 59 was 5.7 hours and 6.5 hours, respectively [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: TF-1 bone marrow cells Tested Concentrations: 0.1, 1, 10, 100, 1000 nM Incubation Duration: 6 hrs (hours) Experimental Results: Inhibition of Fgr autophosphorylation in TF-1 cells. |
| Animal Protocol |
Animal/Disease Models: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice and human MV4-11 AML cells [1]: 1 and 10 mg/kg
Route of Administration: oral; continued for three weeks Experimental Results: Elimination of AML in mouse model AML cells in the spleen and peripheral blood, while Dramatically suppressing bone marrow involvement. |
| References |
| Molecular Formula |
C₃₂H₃₄F₃N₅O₄
|
|---|---|
| Molecular Weight |
609.638678073883
|
| Exact Mass |
609.256
|
| CAS # |
1315330-17-6
|
| Related CAS # |
TL02-59 dihydrochloride;2415263-06-6
|
| PubChem CID |
71254350
|
| Appearance |
White to off-white solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
630.5±55.0 °C at 760 mmHg
|
| Flash Point |
335.1±31.5 °C
|
| Vapour Pressure |
0.0±1.8 mmHg at 25°C
|
| Index of Refraction |
1.603
|
| LogP |
5.22
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
44
|
| Complexity |
923
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
AMHWQBGAKJESFB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C32H34F3N5O4/c1-5-39-10-12-40(13-11-39)18-22-8-9-23(15-25(22)32(33,34)35)38-30(41)21-7-6-20(2)27(14-21)44-31-24-16-28(42-3)29(43-4)17-26(24)36-19-37-31/h6-9,14-17,19H,5,10-13,18H2,1-4H3,(H,38,41)
|
| Chemical Name |
3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]-N-[4-[(4-ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methylbenzamide
|
| Synonyms |
TL02-59 TL02 59 TL0259
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~205.04 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
