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SCH-1473759 hydrochloride

Catalog No. T12864   CAS 1094067-13-6

SCH-1473759 hydrochloride is an inhibitor of aurora(aurora A and B with IC50s of 4 and 13 nM, respectively).

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SCH-1473759 hydrochloride Chemical Structure
SCH-1473759 hydrochloride, CAS 1094067-13-6
Pack Size Availability Price/USD Quantity
2 mg 5 days $ 113.00
5 mg 5 days $ 217.00
10 mg 5 days $ 380.00
1 mL * 10 mM (in DMSO) 5 days $ 229.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SCH-1473759 hydrochloride is an inhibitor of aurora(aurora A and B with IC50s of 4 and 13 nM, respectively).
Targets&IC50 Aurora A:4 nM, Aurora B:13 nM
In vitro SCH-1473759 directly binds to aurora A and B(Kds of 20 and 30 nM, respectively), also inhibits the Src family of kinases with IC50 less than 10 nM, Chk1 with IC50 of 13 nM, VEGFR2 with IC50 of 1 nM), and IRAK4 with IC50 of 37 nM. SCH 1473759 inhibits tumor cell lines from different tissues (breast, ovarian, prostate, lung, colon, brain, gastric, renal, skin, and leukemia). The most sensitive cell lines includ A2780, LNCap, N87, Molt4, K562, and CCRF-CEM with IC50 values <5 nM[2].
In vivo SCH-1473759(5 mg/kg ,ip, bid) was well tolerated in the continuous dosing regimen and showed 50% tumor growth inhibition (TGI) on day 16. SCH-1473759(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 showed good exposure in all species, with high clearance rates in rodents and moderate clearance rates in dogs and monkeys.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].
Molecular Weight 463
Formula C20H27ClN8OS
CAS No. 1094067-13-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 70 mg/mL (151.19 mM), sonification is recommended.

TargetMolReferences and Literature

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. 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.

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Keywords

SCH-1473759 hydrochloride 1094067-13-6 Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase SCH1473759 Hydrochloride inhibit SCH1473759 Inhibitor SCH 1473759 SCH 1473759 Hydrochloride SCH1473759 hydrochloride SCH 1473759 hydrochloride SCH-1473759 Hydrochloride SCH-1473759 inhibitor

 

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