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Purity: ≥98%
SU5402 (SU-5402; SU 5402) is a multi-targeted RTK (receptor tyrosine kinase) inhibitor with potential antineoplastic activity. It has IC50s of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ inhibition, respectively.
| Targets |
VEGFR2 (IC50 = 20 nM); FGFR1 (IC50 = 30 nM); PDGFRβ (IC50 = 510 nM)
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| ln Vivo |
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| Enzyme Assay |
The catalytic domain of FGF-R1 and Flk-1/KDR is expressed as GST fusion proteins after baculoviruses with altered genomes infect Spodoptera frugiperda (sf9) cells. Using glutathione sepharose chromatography, infected sf9 cell lysates are purified to homogeneity for GST-FGFR1 and GST-Flk1. In 96-well microtiter plates, 2.0 μg of a polyGlu-Tyr peptide (4:1) in 0.1 mL of PBS per well is coated overnight before the assays are carried out. The diluted purified kinases are introduced to each test well at a rate of 5 ng of GST fusion protein per 0.05 mL volume buffer using kinase assay buffer (100 mM Hepes pH 7.5, 100 mM NaCl, and 0.1 mM sodium orthovanadate). Test compounds are added to test wells (0.025 mL/well) after being diluted in 4% DMSO. To start the kinase reaction, add 0.025 mL of 40 μM ATP/40 mM MnCl2. Shake the plates for 10 minutes, and then add 0.025 mL of 0.5 M EDTA to stop the reaction. The final concentration of ATP was 10 μM, which is twice the Km value of ATP as determined experimentally. MnCl2 and no ATP are added to the negative control wells. Three rounds of washing are performed on the plates using 10 mM Tris pH 7.4, 150 mM NaCl, and 0.05% Tween-20 (TBST). For one hour, the wells are filled with a 1:10000 dilution of rabbit polyclonal anti-phosphotyrosine antiserum in TBST. After that, TBST is used to wash the plates three times. Then, for one hour, each well received a conjugate of goat anti-rabbit antiserum and horseradish peroxidase. After three TBST washes of the plates, 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) is added to detect the peroxidase reaction. After allowing the assay's color readout to develop for 20 to 30 minutes, it is read using a 410 nM test filter on a Dynatech MR5000 ELISA plate reader.
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| Cell Assay |
The tumor cell lines that are utilized for the in vitro growth are grown in medium with 5–10% CO2 at 37°C. One day after the start of the culture, SU5416 is serially diluted in media containing DMSO (<0.5%) and added to tumor cell cultures. The sulforhodamine B method is used to measure the growth of the cells after 96 hours. Using four-parameter analysis and curve fitting, IC50s are determined.
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| Animal Protocol |
Mice: For one week, intraperitoneal injections of DMSO or SU 5402 (dissolved in DMSO at a concentration of 6 mg/mL) at 25 mg/kg body weight are given to male ΔF508 mice (CFTRtm1Eur on a 129/FVB background) and their wild-type littermates, aged 9–12 weeks. Every day, the dosages are modified based on the mice's weight. Afterwards, isoflurane is breathed into the mice to induce anesthesia until the procedure is completed. To prevent potential cholinergic stimulation of the salivary gland, 50 μL of the cholinergic antagonist atropine (1 mM) is subcutaneously injected into the right cheek. For four minutes, the injected cheek is pressed up against a tiny strip of filter paper. The same location is then subinjected with isoprenaline (10 mM, 37.5 μL) to elicit an adrenergic secretion of saliva (time 0). For thirty minutes, replace the filter strips (pre-weighed in an Eppendorf tube) every five minutes. After the collection is complete, the weight of all six filter strips is measured, and the results are normalized to mg/g body weight.
Rats: Adult male Wistar rats (200–250 g) are given MCT (60 mg/kg s.c.) and left untreated for 21 dayIn order to evaluate the possible impact of the FGFR1 inhibitor SU 5402 on established PH, adult male Wistar rats weighing 200–250 g are administered MCT (60 mg/kg s.c.), allowed to go untreated for 21 days, and then split into two groups at random (10 animals per group): one group receives treatment with SU 5402 (25 mg/kg/day), while the other group receives no treatment from day 21 to day 42. Every treatment is administered intravenously (s.c.) once daily. |
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| References | ||
| Additional Infomation |
SU5402 is an oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 3-(2-carboxyethyl)-4-methyl-1H-pyrrol-2-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1. It has a role as a fibroblast growth factor receptor antagonist. It is a monocarboxylic acid, a member of pyrroles and a member of oxindoles. It is functionally related to a 3-methyleneoxindole.
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| Molecular Formula |
C17H16N2O3
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| Molecular Weight |
296.32
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| Exact Mass |
296.116
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| Elemental Analysis |
C, 68.91; H, 5.44; N, 9.45; O, 16.20
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| CAS # |
215543-92-3
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| Related CAS # |
SU 5402;215543-92-3
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| PubChem CID |
5289418
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| Appearance |
Orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
592.6±50.0 °C at 760 mmHg
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| Melting Point |
>222ºC (dec.)
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| Flash Point |
312.2±30.1 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.688
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| LogP |
2.03
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
488
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCC1=C(NC=C1C)/C=C2C(NC3=C\2C=CC=C3)=O)O
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| InChi Key |
JNDVEAXZWJIOKB-JYRVWZFOSA-N
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| InChi Code |
InChI=1S/C17H16N2O3/c1-10-9-18-15(11(10)6-7-16(20)21)8-13-12-4-2-3-5-14(12)19-17(13)22/h2-5,8-9,18H,6-7H2,1H3,(H,19,22)(H,20,21)/b13-8-
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| Chemical Name |
3-[4-methyl-2-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL | |
| 5 mM | 0.6749 mL | 3.3747 mL | 6.7495 mL | |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 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.
NIH 3T3 Flk-1 cells (A) or NIH 3T3 platelet-derived growth factor β cells (B) grown to confluency were preincubated with SU5416 at concentrations ranging from 0.05 to 50 μm for 1 h at 37°C. Cancer Res. 1999 Jan 1;59(1):99-106. |
A375 cells (3 × 106) were implanted subcutaneous into the hindflank region of female BALB/c nu/nu mice 8–12 weeks of age. Cancer Res. 1999 Jan 1;59(1):99-106. |
Rat C6 glioma cells were surgically implanted (0.5 × 106 cells/animal) under the serosa of the colon in BALB/c nu/nu mice. Beginning 1 day after implantation, animals were treated once daily with a 50 μl i.p. bolus injection of either SU5416 at 25 mg/kg/day in DMSO or DMSO alone for 16 days. On day 16 after implantation, animals were euthanized, and their local tumors in the colon were first quantitated by measurement using venier calipers and then harvested. Cancer Res. 1999 Jan 1;59(1):99-106. |
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