| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
PDGFR; Flk-1
SU-4312 targets VEGFR kinase (Flk-1/KDR) and PDGFR kinase. It inhibits the activated VEGFR kinase with an IC₅₀ of 0.4 μM and the unactivated kinase with an IC₅₀ of 0.04 μM. It also inhibits neuronal nitric oxide synthase (nNOS) and exhibits neuroprotection against NO-mediated neurotoxicity. The compound's selectivity for VEGFR over PDGFR (approximately 48-fold) makes it a useful tool for studying VEGFR-specific signaling pathways. |
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| ln Vitro |
It has been demonstrated that receptor tyrosine kinases (RTKs) are crucial mediators of cellular signal transduction in cells. It has been demonstrated that numerous RTKs are oncogene products, indicating their involvement in the transformation process linked to malignancies in humans[1].
In vitro, SU-4312 has been demonstrated to inhibit receptor tyrosine kinases (RTKs) that are crucial mediators of cellular signal transduction. Many RTKs are oncogene products, indicating their involvement in the transformation process linked to malignancies. SU-4312 selectively and directly inhibits neuronal NOS, providing an unexpected defense against MPP(+)-induced neurotoxicity. Its ability to inhibit VEGFR and PDGFR makes it a valuable tool for studying angiogenesis and cell proliferation. |
| ln Vivo |
In vivo, SU-4312 is used in skin and cosmetic research to study angiogenesis and microcirculation. It has been used to investigate the role of VEGFR signaling in various pathological conditions, including cancer and inflammatory diseases. However, detailed in vivo efficacy and pharmacokinetic data for SU-4312 are not extensively published. Its primary application is as a research tool in cell-based and biochemical assays.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for SU-4312 typically involve evaluating its inhibitory activity against purified VEGFR kinase (Flk-1/KDR) using radiometric or fluorescence-based kinase activity assays. The compound is incubated with the kinase, ATP, and a substrate peptide, and the phosphorylation of the substrate is measured. IC₅₀ values are determined for both the activated and unactivated forms of the kinase to assess the mechanism of inhibition.
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| Cell Assay |
For in vitro cell-based assays, SU-4312 is dissolved in DMSO and applied to cultured cells such as endothelial cells or cancer cells at concentrations ranging from 0.1-50 µM. The effects on cell proliferation, migration, and tube formation are assessed. The inhibition of VEGFR and PDGFR signaling is confirmed by Western blotting for phosphorylation of the receptors and downstream signaling molecules.
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| Animal Protocol |
In vivo animal studies for SU-4312 are typically conducted in rodent models of angiogenesis or cancer. The compound is administered orally or intraperitoneally at doses ranging from 1-50 mg/kg. Efficacy is evaluated by measuring tumor growth, vascular density, or other angiogenesis-related endpoints. However, detailed in vivo data for SU-4312 are not extensively published in the public domain.
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| ADME/Pharmacokinetics |
SU-4312 has a molecular formula of C₁₇H₁₆N₂O and a molecular weight of 264.32 g/mol. It is soluble in DMSO (30 mg/mL) and is typically stored as a powder at 2-8°C. The compound has a melting point of 225-232°C and is stable for up to one year from the date of purchase.
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| Toxicity/Toxicokinetics |
SU-4312 is considered to have a manageable toxicity profile for research use. It is classified as an irritant (Xi) with risk statements R36/37/38 (irritating to eyes, respiratory system, and skin). Appropriate safety precautions, including the use of personal protective equipment, should be followed when handling the compound.
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| References | |
| Additional Infomation |
See also: 3-(4-dimethylaminobenzylidene)-2-indolineone (note moved to).
SU-4312 is a potent and selective inhibitor of VEGFR and PDGFR tyrosine kinases used as a research tool to study angiogenesis, cancer, and neuroprotection. It is also known as DMBI and NSC 86429. SU-4312 is not approved for clinical use and is intended for research purposes only. It is supplied by various research chemical suppliers for non-human use. |
| Molecular Formula |
C17H16N2O
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|---|---|
| Molecular Weight |
264.328
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| Exact Mass |
264.126
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| Elemental Analysis |
C, 77.25; H, 6.10; N, 10.60; O, 6.05
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| CAS # |
5812-07-7
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| Related CAS # |
5812-07-7
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| PubChem CID |
6450842
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| Appearance |
Yellow solid powder
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| Density |
1.219g/cm3
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| Boiling Point |
497.1ºC at 760 mmHg
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| Flash Point |
254.5ºC
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| Index of Refraction |
1.683
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| LogP |
3.383
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
394
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)C1=CC=C(C=C1)C=C2C3=CC=CC=C3NC2=O
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| InChi Key |
UAKWLVYMKBWHMX-PTNGSMBKSA-N
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| InChi Code |
InChI=1S/C17H16N2O/c1-19(2)13-9-7-12(8-10-13)11-15-14-5-3-4-6-16(14)18-17(15)20/h3-11H,1-2H3,(H,18,20)/b15-11-
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| Chemical Name |
(3Z)-3-[[4-(dimethylamino)phenyl]methylidene]-1H-indol-2-one
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| Synonyms |
NSC 86429; NSC-86429; NSC86429; SU4312; DMBI; SU-4312; SU 4312
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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 Note: This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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) |
DMSO: ~50 mg/mL (~189.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (7.87 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7831 mL | 18.9157 mL | 37.8315 mL | |
| 5 mM | 0.7566 mL | 3.7831 mL | 7.5663 mL | |
| 10 mM | 0.3783 mL | 1.8916 mL | 3.7831 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.
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