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Cell Cycle/Checkpoint Aurora Kinase SCH-1473759 hydrochloride

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).

SCH-1473759 hydrochloride, CAS 1094067-13-6
Pack Size Availability Price/USD Quantity
2 mg inquiry 180.00
5 mg inquiry 278.00
10 mg inquiry 395.00
50 mg inquiry 976.00
100 mg inquiry 1421.00
200 mg inquiry inquiry
500 mg inquiry inquiry
1 mL * 10 mM (in DMSO) inquiry 283.00
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Purity 98.00%
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 :ic50 4 nM,   Aurora B :ic50 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

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 70 mg/mL (151.19 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References 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.

Related Products

Related compounds with same targets
SP-146 Aurora Kinase Inhibitor III SNS-314 Mesylate Aurora inhibitor 1 SCH-1473759 AZD1152 MBM-17S MBM-17

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