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| | 1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl- Basic information |
| Product Name: | 1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl- | | Synonyms: | CS-662;1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl-;SCH1473759;SCH1473759/SCH-1473759;2-(Ethyl((5-((6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)amino)isothiazol-3-yl)methyl;2-(Ethyl((5-((6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl)aMino)isothiazol-3-yl)Methyl)aMino)-2-Methylpropan-1-ol;2-(Ethyl((5-((6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)amino)isothiazol-3-yl)met;2-[Ethyl[[5-[[6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-3-isothiazolyl]methyl]amino]-2-methyl-1-propanol | | CAS: | 1094069-99-4 | | MF: | C20H26N8OS | | MW: | 426.54 | | EINECS: | | | Product Categories: | | | Mol File: | 1094069-99-4.mol | ![1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl- Structure](CAS/GIF/1094069-99-4.gif) |
| | 1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl- Chemical Properties |
| density | 1.40±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Powder | | pka | 12.67±0.50(Predicted) | | color | White to yellow |
| | 1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl- Usage And Synthesis |
| Uses | SCH-1473759 is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively. | | in vivo | SCH-1473759 at a low dose of 5 mg/kg (ip, bid) is well-tolerated in a continuous dosing schedule and shows 50% tumor growth inhibition(TGI) on day 16. A higher dose of 10mg/kg(ip, bid) is well-tolerated in an intermittent schedule (5 days on, 5 days off) and gave 69% TGI on day 16. SCH-1473759 shows good exposure in all species with the clearance being high in rodents and moderate in dog and monkey. The half-life is also moderate, but the tissue distribution is high[1]. SCH 1473759 dose- and schedule-dependent anti-tumor activity in four human tumor xenograft models. Further, the efficacy is enhanced in combination with taxanes and found to be most efficacious when SCH 1473759 is dosed 12-h post-taxane treatment[2]. | | IC 50 | Aurora A: 4 nM (IC50); Aurora B: 13 nM (IC50) | | 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. DOI:10.1021/ml100063w
[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. DOI:10.1007/s00280-011-1568-1 |
| | 1-Propanol, 2-[ethyl[[5-[[6-Methyl-3-(1H-pyrazol-4-yl)iMidazo[1,2-a]pyrazin-8-yl]aMino]-3-isothiazolyl]Methyl]aMino]-2-Methyl- Preparation Products And Raw materials |
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