SU 5402 [215543-92-3]
Cat# HY-10407-10mg
Size : 10mg
Brand : MedChemExpress
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.
For research use only. We do not sell to patients.
SU 5402 Chemical Structure
CAS No. : 215543-92-3
This product is a controlled substance and not for sale in your territory.
Based on 9 publication(s) in Google Scholar
Other Forms of SU 5402:
- SU 5402 (GMP) Get quote
View All VEGFR Isoform Specific Products:
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Description |
SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively. |
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IC50 & Target[1] |
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In Vitro |
SU 5402 is cocrystallized with the catalytic domain of FGF-R1 (flg-1) and is found to inhibit tyrosine phosphorylation of VEGF-R2 (Flk-1/KDR) and PDGF-R in NIH 3T3 cells with IC50 values of 0.4 and 60.9 μM, respectively[1]. In order to investigate whether phosphorylation of PKM2 and LDHA is mediated in FGFR1-specific manner, FTC-133 are treated with receptor tyrosine kinase inhibitors Dovitinib and SU 5402 (SU-5402). Dovitinib treatment results in significant decrease of phosphorylation status at a concentration of 100 nM after four hours of incubation for both PKM2 and LDHA. No significant changes are seen when administered at concentrations of 1 nM and 10 nM. SU 5402 administration leads to a sigificant decrease of PKM2 and LDHA phosphorylation at a concentration of 20 μM[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Inhibition of FGFR1 with SU 5402 (SU5402) administered to ΔF508-CFTR homozygous mice results in partial ΔF508-CFTR rescue, as shown by an increase in saliva secretion, a surrogate "sweat test" assay in mice. As salivary secretion is often sex dependent, only male mice are chosen for these experiments. Our results indicate that treatment of the ΔF508-CFTR mice with SU 5402 restores the saliva secretion level to ~10% of that observed for the wild-type CFTR mice, which suggests that SU 5402 can have therapeutic benefits to Cystic Fibrosis (CF)[3]. The selective FGFR1 inhibitor SU 5402 (SU5402) prevents and/or reverses PH induced by MCT (monocrotaline) in rats. In rats treated with SU 5402 on days 21 to 42 after the MCT injection, evaluations on day 42 show marked decreases in pulmonary artery pressure (PAP), RV/(LV+S), and distal artery muscularization compare with rats treated with the vehicle (saline)[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Molecular Weight |
296.32 |
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Formula |
C17H16N2O3 |
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CAS No. |
215543-92-3 |
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Appearance |
Solid |
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Color |
Light brown to orange |
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SMILES |
O=C(CCC1=C(NC=C1C)/C=C2C(NC3=C\2C=CC=C3)=O)O |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : ≥ 30 mg/mL (101.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Purity & Documentation |
Purity: 99.38% |
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References |
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Complete Stock Solution Preparation Table
*
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 3.3747 mL | 16.8736 mL | 33.7473 mL | 84.3682 mL |
5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | 16.8736 mL | |
10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL | 8.4368 mL | |
15 mM | 0.2250 mL | 1.1249 mL | 2.2498 mL | 5.6245 mL | |
20 mM | 0.1687 mL | 0.8437 mL | 1.6874 mL | 4.2184 mL | |
25 mM | 0.1350 mL | 0.6749 mL | 1.3499 mL | 3.3747 mL | |
30 mM | 0.1125 mL | 0.5625 mL | 1.1249 mL | 2.8123 mL | |
40 mM | 0.0844 mL | 0.4218 mL | 0.8437 mL | 2.1092 mL | |
50 mM | 0.0675 mL | 0.3375 mL | 0.6749 mL | 1.6874 mL | |
60 mM | 0.0562 mL | 0.2812 mL | 0.5625 mL | 1.4061 mL | |
80 mM | 0.0422 mL | 0.2109 mL | 0.4218 mL | 1.0546 mL | |
100 mM | 0.0337 mL | 0.1687 mL | 0.3375 mL | 0.8437 mL |