| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| Targets |
IC50: 4.29 μM (tubulin polymerization)[1]
|
|---|---|
| ln Vitro |
S516 exhibits strong cytotoxicity against HL-60, HCT116, and HCT15 cells, with IC50s of 4.8 nM, 42.8 nM, and 24.9 nM, respectively[1]. S516 (Compound 22; 30 nM; 16 hours; HL60 cells) treatment results in a considerable arrest of cells at the G2/M phase, which is followed by apoptosis and the loss of the G0/G1 phase simultaneously[1].
|
| ln Vivo |
In human LX-1 lung cancer and CX-1 colon cancer mouse xenografts, S516 (Compound 22; 5–10 mg/kg; intraperitoneal injection; mice) therapy exhibits encouraging anticancer activity (inhibition ratio (IR)> 63%)[1].
|
| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: HL60 cells Tested Concentrations: 30 nM Incubation Duration: 16 hrs (hours) Experimental Results: Caused significant arrest of cells at the G2/M phase, resulting in apoptosis with concomitant loss of G0/G1 phase. |
| Animal Protocol |
Animal/Disease Models: Mice bearing 3LL lung cancer[1]
Doses: 5 mg/kg, 10 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Had promising antitumor activity (inhibition ratio (IR)> 63%). |
| References |
[1]. Lee J, et al. Identification of CKD-516: a potent tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors. J Med Chem. 2010 Sep 9;53(17):6337-54.
|
| Molecular Formula |
C21H19N5O4S
|
|---|---|
| Molecular Weight |
437.47
|
| CAS # |
1016543-77-3
|
| Related CAS # |
Valecobulin;1188371-47-2;Valecobulin hydrochloride;1240321-53-2
|
| SMILES |
S1C(N)=NC(=C1)C1=CC=C(C(C2C=C(C(=C(C=2)OC)OC)OC)=O)C(=C1)N1C=NC=N1
|
| 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) |
DMSO : 12.5 mg/mL (28.57 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 12.5 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 | 2.2859 mL | 11.4294 mL | 22.8587 mL | |
| 5 mM | 0.4572 mL | 2.2859 mL | 4.5717 mL | |
| 10 mM | 0.2286 mL | 1.1429 mL | 2.2859 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
