ChemicalBook--->CAS DataBase List--->618430-39-0

618430-39-0

618430-39-0 Structure

618430-39-0 Structure
IdentificationBack Directory
[Name]

SB-743291
[CAS]

618430-39-0
[Synonyms]

SB921
SB-921
GSK-921
SB-743291
GSK-743921
SB-743921 free base
SB 743921 free base,SB743921 free base
N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide
N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxo-4H-chromen-2-yl)-2-methylpropyl]-4-methylbenzamide
BenzaMide, N-(3-aMinopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylMethyl)-4H-1-benzopyran-2-yl]-2-Methylpropyl]-4-Methyl-
[Molecular Formula]

C31H33ClN2O3
[MDL Number]

MFCD22628880
[MOL File]

618430-39-0.mol
[Molecular Weight]

517.06
Chemical PropertiesBack Directory
[Boiling point ]

683.0±55.0 °C(Predicted)
[density ]

1.216±0.06 g/cm3(Predicted)
[pka]

9.73±0.10(Predicted)
Hazard InformationBack Directory
[Uses]

SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 free base can induce mitotic arrest, block cell cycle progression, induce apoptosis, and can be used in the research of myeloma, leukemia and other diseases[1][2].
[in vivo]

SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts[3].

[References]

[1] Jeffrey R. Jackson, et al. A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. First AACR International Conference on Molecular Diagnostics in Cancer Therapeutic Development, Sep 12-15, 2006.
[2] Yin Y, et al. Kinesin spindle protein inhibitor SB743921 induces mitotic arrest and apoptosis and overcomes imatinib resistance of chronic myeloid leukemia cells. Leuk Lymphoma. 2015 Jun;56(6):1813-20. DOI:10.3109/10428194.2014.956319
[3] Good JA, et al. Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models. J Med Chem. 2013 Mar 14;56(5):1878-93. DOI:10.1021/jm3014597
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