| Identification | Back Directory | [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- | [CAS]
1094069-99-4 | [Synonyms]
CS-662
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)met
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]-3-isothiazolyl]methyl]amino]-2-methyl-1-propanol
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- | [Molecular Formula]
C20H26N8OS | [MDL Number]
MFCD18251446 | [MOL File]
1094069-99-4.mol | [Molecular Weight]
426.54 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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