Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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ln Vitro |
Aurora A and B are directly bound by SCH-1473759, with a Kd of 20 and 30 nM, respectively. Additionally, the Src kinase family (IC50<10 nM), Chk1 (IC50=13 nM), VEGFR2 (IC50=1 nM), and IRAK4 (IC50=37 nM) are all inhibited by SCH-1473759. IC50>1000 nM) against 34 additional kinases from various kinome families reveals no discernible action. With an IC50 of 6 nM, SCH-1473759 suppresses the growth of HCT116 cells[1]. Tumor cell lines from many tissues (breast, ovary, prostate, lung, colon, brain, stomach, kidney, skin, and leukemia) are inhibited by SCH 1473759. With IC50 values less than 5 nM, A2780, LNCap, N87, Molt4, K562, and CCRF-CEM are the most sensitive cell lines [2].
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ln Vivo |
At day 16, 50% tumor growth inhibition (TGI) was shown by SCH-1473759 at a low dose of 5 mg/kg (ip, bid), which was well tolerated in a continuous dosing regimen. An intermittent schedule of five days on and five days off allowed for good tolerance of the larger dose of 10 mg/kg (ip, bid), which produced a TGI of 69% on day sixteen. With a high clearance in rats and a moderate clearance in dogs and monkeys, SCH-1473759 demonstrated good exposure in all species. There is a high tissue dispersion despite the moderate half-life [1]. In four human tumor xenograft models, SCH 1473759 exhibits dose- and schedule-dependent anticancer efficacy. Furthermore, SCH 1473759 is more effective when used in conjunction with taxanes; it was discovered that the optimal time to take it was 12 hours following taxane treatment [2].
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References |
[1]. Yu T, et al. Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core. ACS Med Chem Lett. 2010 Jun 7;1(5):214-8.
[2]. Basso AD, et al. SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors. Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33 |
Molecular Formula |
C32H42N4O5
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Molecular Weight |
562.69968
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CAS # |
1094067-13-6
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Related CAS # |
SCH-1473759;1094069-99-4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
[H]Cl.CC1=CN2C(C(NC3=CC(CN(C(C)(CO)C)CC)=NS3)=N1)=NC=C2C4=CNN=C4
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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) |
H2O : ~8.33 mg/mL (~17.99 mM)
DMSO : ~7.14 mg/mL (~15.42 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.71 mg/mL (1.53 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 7.1 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: ≥ 0.71 mg/mL (1.53 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 7.1 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 | 1.7771 mL | 8.8857 mL | 17.7715 mL | |
5 mM | 0.3554 mL | 1.7771 mL | 3.5543 mL | |
10 mM | 0.1777 mL | 0.8886 mL | 1.7771 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.