SCH-1473759 - CAS 1094069-99-4
Catalog number: 1094069-99-4
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C20H26N8OS
Molecular Weight:
426.54
COA:
Inquire
Targets:
Aurora Kinase
Description:
SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and genetic backgrounds. SCH-1473759 demonstrated potent mechanism-based activity, and activity was shown to be enhanced in combination with taxanes and KSP inhibitors.
Purity:
0.98
Appearance:
Light yellow to yellow solid
Synonyms:
SCH1473759; SCH 1473759.
MSDS:
Inquire
InChIKey:
RHGZQGXELRMGES-UHFFFAOYSA-N
InChI:
InChI=1S/C20H26N8OS/c1-5-27(20(3,4)12-29)11-15-6-17(30-26-15)25-18-19-21-9-16(14-7-22-23-8-14)28(19)10-13(2)24-18/h6-10,29H,5,11-12H2,1-4H3,(H,22,23)(H,24,25)
Canonical SMILES:
CCN(CC1=NSC(=C1)NC2=NC(=CN3C2=NC=C3C4=CNN=C4)C)C(C)(C)CO
Current Developer:
Merck.
1.A simple and rapid UHPLC-MS/MS method for the quantitation of the dual aurora kinase A/B inhibitor SCH-1473759 in murine plasma.
Ferraz Nogueira Filho MA;Peer CJ;Nguyen J;McCalla A;Helman L;Figg WD J Pharm Biomed Anal. 2017 Jan 5;132:223-226. doi: 10.1016/j.jpba.2016.10.003. Epub 2016 Oct 5.
The Aurora kinase family facilitates cell division through various processes and is overexpressed in a wide variety of human cancers, leading to aneuploidy. For that reason, these enzymes are currently targets of a rising class of anticancer drugs, with some molecules already in therapeutic use. In this study, a new UHPLC-MS/MS method was developed and validated to quantitate a new pan Aurora kinase inhibitor still in preclinical development, SCH-1473759. This bioanalytical method employed a liquid-liquid extraction from plasma using ethyl acetate before evaporation. Calibration range encompassed 0.5-2500ng/mL. The inter- and intra-day accuracy and precision were assessed over five quality control levels; all within limits required by the FDA guidelines. Assay applicability was demonstrated in a first-in-animals study with oral administration, where the maximum plasma concentration (34ng/mL) occurred at 1h, the half-life (1h) was consistent with a previous IV study, and oral bioavailability was poor (F=0.002).
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Aurora Kinase Products


CAS 1158838-45-9 Aurora A Inhibitor I

Aurora A Inhibitor I
(CAS: 1158838-45-9)

Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM. It is 1000-fold more selective for Aurora A than Aurora B.

CAS 656820-32-5 Reversine

Reversine
(CAS: 656820-32-5)

Reversine is a small molecule developed by the group of Peter G. Schultz, used for stem cell dedifferentiation. Reversine is also a novel Aurora kinases inhibit...

CAS 898280-07-4 XL228

XL228
(CAS: 898280-07-4)

XL228 is a protein kinase inhibitor targeting IGF1R, the Aurora kinases, FGFR1-3, ABL and SRC family kinases.

CAS 934353-76-1 ENMD-2076

ENMD-2076
(CAS: 934353-76-1)

ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has be...

CAS 827318-97-8 Danusertib

Danusertib
(CAS: 827318-97-8)

Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Aurora kinase inhibitor PHA-739358 binds to and inhibits the A...

CAS 1094069-99-4 SCH-1473759

SCH-1473759
(CAS: 1094069-99-4)

SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and gen...

CAS 1291074-87-7 ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid
(CAS: 1291074-87-7)

ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selec...

CAS 885325-71-3 MK-8745

MK-8745
(CAS: 885325-71-3)

MK-8745 is a novel Aurora-A specific inhibitor. MK8745 induced apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lin...

Chemical Structure

CAS 1094069-99-4 SCH-1473759

Quick Inquiry

Verification code

Featured Items