| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
The area and number of H1299 and H460 cells grow in a concentration-dependent manner when exposed to salty (0, 3, 10, 30 nM) for 24 hours [2]. Salted ilotasertib (1–1000 nM) exhibits antiproliferative properties [2]. Examine[2]
|
|---|---|
| ln Vivo |
In SCID mice bearing MV-4-11 tumors, ilotinib hydrochloride (6.25, 12.5, and 25 mg/kg; interface) exhibited anti-tumor efficacy, with TGIs of 80 at 6.25, 12.5, and 25 mg/kg, correspondingly. With TGIs of 38% and 59%, respectively, iloratib hydrochloride (6.25, 12.5, 25 mg/kg; po) demonstrated tumor anti-tumor efficacy in SCID mice bearing confirmed SKM-1 tumors. 80 percent. Histone H3 phosphorylation in blood-borne tumor cells is inhibited by imolipartib hydrochloride (0, 3.75, 7.5, and 15 mg/kg; ip) after 4–8 hours [2]. In mice, ilotinib hydrochloride (0.2 mg/kg; IV) demonstrates anti-VEGF efficacy [2]. Mice treated with imipratim hydrochloride (20 mg/kg; sidewall once weekly for 3 weeks) demonstrated anticancer action.
|
| Cell Assay |
Test[2]
Cell Types: H1299, H460 Cell Tested Concentrations: 0, 3, 10, 30 nM Incubation Duration: 24 hrs (hours) Experimental Results: The degree and number of induced polyploid cells increased in a concentration-dependent manner, with EC50S of 5 and 10 nM respectively. Targets H1299 and H460 cells. Cell proliferation assay[2] Cell Types: MV-4-11, SEM, K562, HCT-15, SW620, H1299, H460 Cell Tested Concentrations: 1-1000 nM Incubation Duration: Experimental Results: Displayed anti-proliferative activity with IC50 of 0.3, 1. 103, 6, 6, 2, and 2 nM for MV-4-11, SEM, K562, HCT-15, SW620, H1299, and H460 cells respectively. |
| Animal Protocol |
Animal/Disease Models: Female SCID/beige mouse[2]
Doses: 25 mg/kg Route of Administration: subcutaneousmini-pump;[2]. 24-hour Experimental Results: Inhibition of histone H3 phosphorylation, tumor drug concentration is related to 50% inhibition of histone H3 phosphorylation. Animal/Disease Models: 22-26 g, female NOD/SCID (severe combined immunodeficient) mouse (multiple myeloma xenograft model (KMS11)) [2] Doses: 20 mg/kg Route of Administration: Po; once a week for 3 weeks Experimental Results: Inhibits tumor growth in mice. |
| References |
[1]. Yi-Chun Wang, et al. Abstract 858: Potent in vivo activity of the aurora kinase inhibitor ABT-348 in human acute myeloid leukemia and myelodysplastic syndrome xenograft models. Cancer Res (2012) 72 (8_Supplement): 858.
[2]. Glaser KB, et al. Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27. |
| Molecular Formula |
C25H22CLFN6O2S
|
|---|---|
| Molecular Weight |
524.997585773468
|
| CAS # |
1847485-91-9
|
| Related CAS # |
Ilorasertib;1227939-82-3
|
| SMILES |
Cl.S1C=C(C2C=CC(=CC=2)NC(NC2C=CC=C(C=2)F)=O)C2C(N)=NC=C(C3C=NN(CCO)C=3)C1=2
|
| 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 : ~41.67 mg/mL (~79.37 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.96 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.96 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 1.9048 mL | 9.5238 mL | 19.0476 mL | |
| 5 mM | 0.3810 mL | 1.9048 mL | 3.8095 mL | |
| 10 mM | 0.1905 mL | 0.9524 mL | 1.9048 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
