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| Targets |
SB-633825 targets TIE2 Tyrosine-protein kinase (TIE2), lymphocyte-oriented kinase (LOK, also known as STK10), and breast tumor kinase (Brk, also known as PTK6). It acts as an ATP-competitive inhibitor for these kinases. It is also studied for its potential to block IGF-1R signaling. These targets are involved in cell growth, angiogenesis, and cancer progression.
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| ln Vitro |
Breast tumor suppressor (Brk; PTK6), inhibitor of inhibitor of casein (LOK; STK10), and TIE2 inhibitor of casein (TIE2) are all inhibited by SB-633825 [1]. At 0.1 μM, SB-633825 reduces the maximal activity of TIE2 to 75% and LOK to 44% [1].
SB-633825 is a potent in vitro inhibitor of its target kinases. It inhibits TIE2 with an IC50 of 3.5 nM, LOK with an IC50 of 66 nM, and BRK with an IC50 of 150 nM. At a concentration of 0.1 μM, it inhibits LOK to 44% of its maximal activity and TIE2 to 75% of its maximal activity. These data confirm its potent and selective inhibitory profile against these kinases in cell-free assays. |
| ln Vivo |
SB-633825 has been shown to inhibit cancer cell growth and angiogenesis in vitro. It is studied for its potential to block IGF-1R signaling, thereby inhibiting tumor growth and inducing apoptosis in cancer cells. Research focuses on its efficacy in treating cancers that are driven by IGF-1R overexpression, suggesting it has been evaluated in relevant in vivo models.
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| Enzyme Assay |
The in vitro kinase inhibition assays for SB-633825 involve measuring its ability to inhibit the activity of purified recombinant kinases. The compound is tested at various concentrations in the presence of ATP and a substrate, and the extent of phosphorylation is measured. The IC50 values of 3.5 nM for TIE2, 66 nM for LOK, and 150 nM for BRK are determined from these assays.
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| Cell Assay |
The in vitro activity of SB-633825 is also evaluated in cell-based assays. The compound's ability to inhibit cancer cell growth is typically measured using cell viability assays in various cancer cell lines. Its effect on angiogenesis can be assessed using endothelial cell tube formation assays. The compound's ability to inhibit downstream signaling pathways, such as those mediated by IGF-1R, can be measured by Western blotting.
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| Animal Protocol |
While specific in vivo protocols are not detailed, SB-633825 has been studied in animal models of cancer. These studies typically involve administering the compound to mice bearing tumor xenografts. Tumor growth inhibition, angiogenesis, and apoptosis are monitored as endpoints. Its potential to block IGF-1R signaling suggests it has been evaluated in models of IGF-1R-driven cancers.
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| ADME/Pharmacokinetics |
SB-633825 has a molecular weight of 483.58 and a molecular formula of C28H25N3O3S. For research purposes, the powder should be stored at -20°C for up to 3 years, and in solvent at -80°C for up to 1 year. It is shipped with blue ice or at ambient temperature. The compound is a potent and ATP-competitive inhibitor of TIE2, LOK, and BRK.
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| Toxicity/Toxicokinetics |
SB-633825 is a multi-kinase inhibitor with potential anticancer activity. Its toxicity profile is not detailed in the provided sources. As with other kinase inhibitors, potential toxicities could be related to on-target effects on normal cells expressing the target kinases (TIE2, LOK, BRK) or off-target effects on other kinases. Thorough preclinical toxicology studies would be necessary for its development as a therapeutic agent.
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| References | |
| Additional Infomation |
SB-633825 (CAS#: 956613-01-7) is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10), and BRK (PTK6) with IC50 values of 3.5 nM, 66 nM, and 150 nM, respectively. It inhibits cancer cell growth and angiogenesis. It is also studied for its potential to block IGF-1R signaling. SB-633825 is a research tool for studying the role of these kinases in cancer and angiogenesis.
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| Molecular Formula |
C28H25N3O3S
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| Molecular Weight |
483.58140540123
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| Exact Mass |
483.161
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| CAS # |
956613-01-7
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| PubChem CID |
44433173
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
35
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| Complexity |
811
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=S(C)(C1C=C(C)C(C2N(C)C(C3C=C4C(C=C(C=C4)OC)=CC=3)=C(C3C=CN=CC=3)N=2)=CC=1)=O
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| InChi Key |
ZDSNJSQTPLXCSG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H25N3O3S/c1-18-15-24(35(4,32)33)9-10-25(18)28-30-26(19-11-13-29-14-12-19)27(31(28)2)22-6-5-21-17-23(34-3)8-7-20(21)16-22/h5-17H,1-4H3
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| Chemical Name |
4-[5-(6-methoxynaphthalen-2-yl)-1-methyl-2-(2-methyl-4-methylsulfonylphenyl)imidazol-4-yl]pyridine
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| Synonyms |
SB633825; SB 633825; SB-633825
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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 : ~9.62 mg/mL (~19.89 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 | 2.0679 mL | 10.3396 mL | 20.6791 mL | |
| 5 mM | 0.4136 mL | 2.0679 mL | 4.1358 mL | |
| 10 mM | 0.2068 mL | 1.0340 mL | 2.0679 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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