| Identification | Back Directory | [Name]
SCH1473759 (HCl salt) | [CAS]
1094067-13-6 | [Synonyms]
SCH-1473759 HCl
SCH1473759 (HCl salt)
SCH-1473759 hydrochloride | [Molecular Formula]
C20H27ClN8OS | [MDL Number]
MFCD18251447 | [MOL File]
1094067-13-6.mol | [Molecular Weight]
463 |
| Hazard Information | Back Directory | [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) | [storage]
Store at -20°C | [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 |
|
| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
|