SB-743921 is a kinesin spindle protein inhibitor with IC50 of 0.2 nM, 0.07 nM, 1.7 nM, 0.06 nM and 14.4 nM in SKOV3, Colo205, MV522, MX1 and P388 cell lines, respectively. SB-743921 selectively inhibits kinesin spindle protein (KSP), an important protein involved in the early stages of mitosis that is expressed in proliferating cells. SB 743921 blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death. SB-743921 has significant efficacy in a broad spectrum of tumor models differing from that of taxanes. The maximum-tolerated dose (MTD) of SB-743921 as a 1-h infusion every 21 days was established as 4 mg/m(2). SB-743921 has entered in a Phase I clinical trial in the treatment of cancer.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 60 mg/mL
Ethanol ≥ 60 mg/mL
Optimized S-Trityl-l-cysteine-Based Inhibitors of Kinesin Spindle Protein with Potent in Vivo Antitumor Activity in Lung Cancer Xenograft Models.
Good JA, et al. J Med Chem. 2013 Mar 14;56(5):1878-93. PMID: 23394180.
A first in human study of SB-743921, a kinesin spindle protein inhibitor, to determine pharmacokinetics, biologic effects and establish a recommended phase II dose.
Holen KD, et al. Cancer Chemother Pharmacol. 2011 Feb;67(2):447-54. PMID: 20461380.
|Related Kinesin Products|
ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor.
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
BAY 1217389 is a potent, and selective inhibitor of the monopolar spindle 1 (MPS1) kinase with an IC50 value less than 10 nM.
Eg5 is a key protein involved in the formation of bipolar spindles.
Monastrol is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles.
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