SCH1473759 (HCl salt)
- Product Name
- SCH1473759 (HCl salt)
- CAS No.
- 1094067-13-6
- Chemical Name
- SCH1473759 (HCl salt)
- Synonyms
- SCH-1473759 HCl;SCH1473759 (HCl salt);SCH-1473759 hydrochloride;SCH-1473759 hydrochloride /1094067-13-6;Aurora Kinase,inhibit,SCH1473759,Inhibitor,SCH 1473759,SCH1473759 hydrochloride,SCH 1473759 hydrochloride,SCH-1473759
- CBNumber
- CB02628389
- Molecular Formula
- C20H27ClN8OS
- Formula Weight
- 463
- MOL File
- 1094067-13-6.mol
SCH1473759 (HCl salt) Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 70 mg/mL (151.19 mM)
- form
- Solid
- color
- White to yellow
N-Bromosuccinimide Price
- Product number
- CS-3477
- Product name
- SCH-1473759hydrochloride
- Purity
- 99.67%
- Packaging
- 2mg
- Price
- $144
- Updated
- 2021/12/16
- Product number
- CS-3477
- Product name
- SCH-1473759hydrochloride
- Purity
- 99.67%
- Packaging
- 5mg
- Price
- $264
- Updated
- 2021/12/16
- Product number
- orb611479
- Product name
- SCH-1473759 hydrochloride
- Packaging
- 5mg
- Price
- $368.9
- Updated
- 2021/12/16
- Product number
- CS-3477
- Product name
- SCH-1473759hydrochloride
- Purity
- 99.67%
- Packaging
- 10mg
- Price
- $384
- Updated
- 2021/12/16
- Product number
- KIN0000833
- Product name
- SCH-1473759 HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $500.65
- Updated
- 2021/12/16
SCH1473759 (HCl salt) Chemical Properties,Usage,Production
Uses
SCH-1473759 hydrochloride 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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