SU5614 |
| Catalog No.GC14582 |
SU5614 est un puissant inhibiteur de FLT3 et induit sélectivement l'arrêt de la croissance, l'apoptose et l'arrêt du cycle cellulaire dans les lignées cellulaires Ba/F3 et AML exprimant un FLT3 activé de manière constitutive.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1055412-47-9
Sample solution is provided at 25 µL, 10mM.
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IC50: 100 nM for FLT3 inhibition
SU5614 is a protein tyrosine kinase inhibitor.
Tyrosine kinases are enzymes for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein.
In vitro: Previous study found that SU5614 could induce growth arrest and apoptosis in c-kit-expressing Kasumi-1, M-07e, and UT-7 cells and inhibited the stem cell factor (SCF)-induced tyrosine phosphorylation of c-kit. Moreover, the sensitivity of Kasumi-1 cells towards the growth inhibitory activity of SU5614 was mainly caused by an autocrine production of SCF, but not by the transforming mutations of c-kit [1].
In vivo: It was found that administration of SU5614, a vascular endothelial growth factor (VEGF) inhibitor, to mice could reduce the levels of VEGF dramatically in BAL fluids 72 h after toluene diisocyanate inhalation. Moreover, consistent with the results obtained from the enzyme immunoassays, Western blot analyses showed that SU5614 reduced the levels of VEGF in the BAL fluid 72 h after toluene diisocyanate inhalation. These results suggested that VEGF might be one of the major determinants of toluene diisocyanate -induced asthma and that the inhibition of VEGF might be a good therapeutic strategy [2].
Clinical trial: Up to now, SU5614 is still in the preclinical development stage.
References:
[1] Spiekermann K,Faber F,Voswinckel R,Hiddemann W. The protein tyrosine kinase inhibitor SU5614 inhibits VEGF-induced endothelial cell sprouting and induces growth arrest and apoptosis by inhibition of c-kit in AML cells. Exp Hematol.2002 Jul;30(7):767-73.
[2] Lee YC,Kwak YG,Song CH. Contribution of vascular endothelial growth factor to airway hyperresponsiveness and inflammation in a murine model of toluene diisocyanate-induced asthma. J Immunol.2002 Apr 1;168(7):3595-600.
| Cas No. | 1055412-47-9 | SDF | |
| Chemical Name | (Z)-5-chloro-3-((3,5-dimethyl-1H-pyrrol-2-yl)methylene)indolin-2-one | ||
| Canonical SMILES | CC(C=C(N1)C)=C1/C([H])=C(C2=O)/C3=C(N2)C=CC(Cl)=C3 | ||
| Formula | C15H13ClN2O | M.Wt | 272.73 |
| Solubility | ≥ 27.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6666 mL | 18.3332 mL | 36.6663 mL |
| 5 mM | 0.7333 mL | 3.6666 mL | 7.3333 mL |
| 10 mM | 0.3667 mL | 1.8333 mL | 3.6666 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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