| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
SU11652 targets receptor tyrosine kinases (RTKs), particularly those involved in angiogenesis and tumor growth. It inhibits VEGFR (vascular endothelial growth factor receptor), FGFR (fibroblast growth factor receptor), PDGFR (platelet-derived growth factor receptor), and Kit. SU11652 is also an inhibitor of sphingomyelin phosphodiesterase.
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| ln Vitro |
Mast cell lines that express the mutant Kit are inhibited in their proliferation by SU11652 (0-1 μM, 0-72 hours) [1]. In cell lines expressing mutant Kit, SU11652 (0-1 μM, 0-72 hours) causes cell cycle arrest and subsequent apoptosis [1].
SU11652 is a potent receptor tyrosine kinase (RTK) inhibitor. It inhibits VEGFR, FGFR, PDGFR, and Kit. SU11652 is a potent Flk-1 antagonist that selectively disrupts the receptor's activation by preventing ligand-induced conformational changes. Specific IC50 values are not extensively detailed in standard reference sources. |
| ln Vivo |
SU11652 has been investigated for its anti-angiogenic and anti-tumor activities. As an RTK inhibitor, it inhibits signaling pathways critical for angiogenesis and tumor growth. SU11652 can be used in the study of spontaneous cancers expressing Kit mutations.
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| Enzyme Assay |
SU11652's inhibitory activity against RTKs can be assessed using in vitro kinase assays. Recombinant RTK enzymes (e.g., VEGFR, FGFR, PDGFR, Kit) are incubated with their respective substrates and ATP in the presence of varying concentrations of SU11652. The amount of phosphorylated substrate is measured to determine the IC50.
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| Cell Assay |
The cellular activity of SU11652 is evaluated in cell-based assays. Cells expressing RTKs (e.g., endothelial cells, cancer cells) are treated with increasing concentrations of SU11652. Cell proliferation, migration, and angiogenesis-related processes such as tube formation are assessed. The effect on RTK phosphorylation is measured by Western blot.
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| Animal Protocol |
Specific in vivo animal experimental protocols for SU11652 are not extensively detailed in standard reference sources. For evaluating its anti-angiogenic and anti-tumor activity, SU11652 would be administered to tumor-bearing mice or models of angiogenesis. Tumor growth, vascular density, and angiogenesis markers would be assessed.
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| ADME/Pharmacokinetics |
SU11652 has a molecular formula of C22H28ClN5O2 and a molecular weight of 429.94. It is a tyrosine kinase inhibitor. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of SU11652 is not extensively documented. As a multi-kinase inhibitor, potential adverse effects may include those related to inhibition of VEGFR, PDGFR, and other RTKs. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References | |
| Additional Infomation |
SU11652 is a pyrrole carboxamide compound formed by the condensation of the carboxyl group of 5-[(Z)-(5-chloro-2-oxo-1,2-dihydroindole-3-methylene)methyl]-2,4-dimethylpyrrole-3-carboxylic acid with the primary amino group of N(1),N(1)-diethylethane-1,2-diamine. It is an EC 2.7.10.1 (receptor protein tyrosine kinase) inhibitor and an EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor. It belongs to the indole ketone class, organochlorine compounds, tertiary amines, and olefins. Functionally, it is related to 3-methyleneindole. SU-11652 is a tyrosine kinase inhibitor.
SU11652 (CAS# 326914-10-7) is a potent receptor tyrosine kinase (RTK) inhibitor. It inhibits VEGFR, FGFR, PDGFR, and Kit. SU11652 is a potent Flk-1 antagonist that inhibits angiogenesis and tumor growth. It is a research tool for studying RTK signaling and cancer. |
| Molecular Formula |
C22H27CLN4O2
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|---|---|
| Molecular Weight |
414.93
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| Exact Mass |
414.182
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| CAS # |
326914-10-7
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| PubChem CID |
5329103
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| Appearance |
Yellow to orange solid powder
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| LogP |
4.378
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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 |
7
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| Heavy Atom Count |
29
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| Complexity |
636
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)CCNC(=O)C1=C(NC(=C1C)/C=C\2/C3=C(C=CC(=C3)Cl)NC2=O)C
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| InChi Key |
XPLJEFSRINKZLC-ATVHPVEESA-N
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| InChi Code |
InChI=1S/C22H27ClN4O2/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28)/b17-12-
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| Chemical Name |
5-[(Z)-(5-chloro-2-oxo-1H-indol-3-ylidene)methyl]-N-[2-(diethylamino)ethyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
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| Synonyms |
SU-11652; SU 11652; SU11652
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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 |
| 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 : ~10 mg/mL (~24.10 mM)
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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 | 2.4100 mL | 12.0502 mL | 24.1005 mL | |
| 5 mM | 0.4820 mL | 2.4100 mL | 4.8201 mL | |
| 10 mM | 0.2410 mL | 1.2050 mL | 2.4100 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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