| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| ln Vitro |
Tubulin/CDC5L-IN-1 (Compound 11i) (48 h) inhibited the proliferation of HeLa, HCT 116, A2780 and A549 cells with IC50 values of 0.046, 0.035, 0.096 and 0.112 μM, respectively [1]. Tubulin/CDC5L-IN-1 showed antiproliferative efficacy in drug-resistant cancer cells with IC50 values ranging from 0.089 to 0.172 μM [1]. Tubulin/CDC5L-IN-1 (1-100 μM, 0-30 mins) inhibited microtubule assembly with an IC50 value of 28.8 μM [1]. Tubulin/CDC5L-IN-1 (0.125-0.05 μM, 24 h) inhibited colony formation in HeLa and HCT 116 cells [1]. Tubulin/CDC5L-IN-1 (0.125-0.1 μM, 12 h) can induce G2/M phase arrest in HCT 116 cells[1]. Tubulin/CDC5L-IN-1 (0.05-0.2 μM, 24 h) can induce apoptosis in HCT 116 cells and produce reactive oxygen species (ROS)[1]. Tubulin/CDC5L-IN-1 (0.05-0.2 μM, 4 h) can inhibit the formation of capillary-like structures in human umbilical vein endothelial cells (HUVECs)[1]. Tubulin/CDC5L-IN-1 (5 μM) can inhibit DNA-dependent protein kinase and cell cycle 7[1].
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|---|---|
| ln Vivo |
Tubulin/CDC5L-IN-1 (Compound 11i) (7.5-20 mg/kg, intraperitoneal injection, every 2 days) inhibited tumor growth in the HCT116 xenograft model [1].
|
| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: HCT 116 cells Tested Concentrations: 0.125, 0.05 and 0.1 μM Incubation Duration: 12 h Experimental Results: Increased cells in the G2/M phase. Increased the phosphorylation level of histone H3 (PHH3) at Ser10. |
| Animal Protocol |
Animal/Disease Models: HCT116 xenograft mice models[1]
Doses: 7.5, 10 and 20 mg/kg Route of Administration: Intraperitoneally injection, every 2 days Experimental Results: Reduced tumor weight and volume. Had no body weight loss. Decreased Ki67-positive cells and reduced tumor microvessel density. Had no histopathological changes in the heart, liver, spleen, lungs, or kidneys. |
| References |
| Molecular Formula |
C28H32N6O8
|
|---|---|
| Molecular Weight |
580.59
|
| CAS # |
3050832-41-9
|
| Appearance |
White to off-white solid powder
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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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~172.24 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.31 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 25.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix thoroughly. Then add 50 μL of Tween-80 to the above system and mix thoroughly. Finally, add 450 μL of physiological saline to bring the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in ddH₂O and bring the volume to 100 mL to obtain a clear and transparent physiological saline solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.31 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 25.0 mg/mL clarified DMSO stock solution to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7224 mL | 8.6119 mL | 17.2239 mL | |
| 5 mM | 0.3445 mL | 1.7224 mL | 3.4448 mL | |
| 10 mM | 0.1722 mL | 0.8612 mL | 1.7224 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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