| Size | Price | Stock | Qty |
|---|---|---|---|
| 2mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
SU 9516 (SU-9516; SU9516), a 3-substituted indolinone, is a potent and selective Cyclin-dependent kinases (CDKs) inhibitor with potential antineoplastic activity. With respective IC50s of 22 nM, 40 nM, and 200 nM, it inhibits CDK2, CDK1, and CDK4. SU 9516 (5 μM) reduced pRb's phosphorylation in RKO cells by 52%, specifically in the cdk2-specific region. In SW480 cells, however, SU9516 (5 μM) significantly reduced the phosphorylation of pRb that is specific to either CDK2 or CDK4, by 64% and 49%, respectively. Moreover, G0-G1 or G2-M block and dose-dependent induction of apoptosis were the outcomes of SU 9516 (5 μM). Time-dependently, SU9516 (5 μM) prevented pRb from dissociating from E2F1 in human colon cancer cells HT-29, SW480, and RKO.
| Targets |
CDK2 (IC50 = 22 nM); CDK1 (IC50 = 40 nM); CDK4 (IC50 = 200 nM); PDGFr (IC50 = 18000 nM)
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| Enzyme Assay |
Polypropylene plates with 96 wells are used for kinase assays. A 40 μL volume containing 10 mM MgCl2, 1 mM DTT, 0.01% Triton X-100, 10% glycerol, and 2 μg of histone H1 at a final concentration of 10 μM [-33P]ATP (0.2 μCi/well) is used in each reaction. 20 μL of the enzyme (6 ng cdk2/well, or 1.6 nM at the end concentration) is added to start the reaction. The enzyme has been diluted 1:50–1:200 in the same buffer and has been left to proceed for one hour at room temperature. 25 μL of the reaction mixture is transferred to P30 phosphocellulose filter mat paper, and the reaction is stopped by adding 0.01 mL of 10% phosphoric acid. The filter mat is air dried, rinsed three times with 1.0% phosphoric acid, and then its radioactivity is measured using a liquid scintillation counter.
|
||
| Cell Assay |
In 96-well plates, RKO and SW480 cells are seeded at a density of 1×104 cells/well in duplicates (n = 6) and left to attach overnight. Following a 24-hour addition of SU9516 at concentrations ranging from 0.05 μM to 50.00 μM, the cells are twice washed with PBS and restocked with full media. Using a modified SRB cytotoxicity assay, the cells are fixed at 0, 4, and 7 days after the drug is removed and their protein levels are measured. After being fixed for one hour in 10% trichloroacetic acid, the cells are cleaned in distilled water and stained for thirty minutes in 0.4% SRB/acetic acid. After solubilizing in 10 mM Tris (pH 9), the cells are rinsed in 0.1% acetic acid and examined at 595 nm using a Bio-Rad 360 microplate reader. Every experiment is run through three times or more.
|
||
| Animal Protocol |
|
||
| References |
|
| Molecular Formula |
C13H11N3O2
|
|
|---|---|---|
| Molecular Weight |
241.25
|
|
| Exact Mass |
241.09
|
|
| Elemental Analysis |
C, 64.72; H, 4.60; N, 17.42; O, 13.26
|
|
| CAS # |
377090-84-1
|
|
| Related CAS # |
|
|
| Appearance |
Solid powder
|
|
| SMILES |
C1=CC=C(C=C1)CC(C2=CC=CC=C2)C(=O)NC3=CN=C(C=C3)C(=O)NC4=CC=CC=C4N
|
|
| InChi Key |
FUOLFAHJLGZFME-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C27H24N4O2/c28-23-13-7-8-14-24(23)31-27(33)25-16-15-21(18-29-25)30-26(32)22(20-11-5-2-6-12-20)17-19-9-3-1-4-10-19/h1-16,18,22H,17,28H2,(H,30,32)(H,31,33)
|
|
| Chemical Name |
N-(2-aminophenyl)-5-(2,3-diphenylpropanoylamino)pyridine-2-carboxamide
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.25 mg/mL (13.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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. Solubility in Formulation 2: ≥ 3.25 mg/mL (13.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 32.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1451 mL | 20.7254 mL | 41.4508 mL | |
| 5 mM | 0.8290 mL | 4.1451 mL | 8.2902 mL | |
| 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA