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-
- 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-
- CAS No.
- 1094069-99-4
- Chemical 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;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]-3-isothiazolyl]methyl]amino]-2-methyl-1-propanol;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;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-
- CBNumber
- CB62550774
- Molecular Formula
- C20H26N8OS
- Formula Weight
- 426.54
- 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- Property
- 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 and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-1341
- Product name
- SCH-1473759
- Purity
- 98.20%
- Packaging
- 2mg
- Price
- $144
- Updated
- 2021/12/16
- Product number
- CS-1341
- Product name
- SCH-1473759
- Purity
- 98.20%
- Packaging
- 5mg
- Price
- $264
- Updated
- 2021/12/16
- Product number
- orb611480
- Product name
- SCH-1473759
- Packaging
- 5mg
- Price
- $368.9
- Updated
- 2021/12/16
- Product number
- CS-1341
- Product name
- SCH-1473759
- Purity
- 98.20%
- Packaging
- 10mg
- Price
- $384
- Updated
- 2021/12/16
- Product number
- KIN0000834
- Product name
- SCH-1473759
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $497.34
- Updated
- 2021/12/16
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,Usage,Production
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
Raw materials
Preparation Products
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- Suppliers
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