SB-743921 free base 

SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a K_i 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].

SB-743921 is a potent inhibitor of Eg5, with a K_i of 0.1 nM^[1].
SB-743921 (1 nM) potently inhibits colony forming cell (CFC) formation of chronic myeloid leukemia (CML) primary cells, but exhibits slight inhibitory activities on the colony-forming ability of normal bone marrow progenitors^[2].
SB-743921 (1-3 nM) induces apoptosis of CML primary CD34⁺ cells, and shows slight effect on normal CD34⁺ cells. SB-743921 in combination with imatinib displays additive anti-proliferative effect in KCL22 and CML CD34⁺ cells. Furthermore, SB-743921 overcomes imatinib resistance in CML cells^[2].
SB-743921 (0.5 nM, 1 nM, 3 nM) inhibits MEK/ERK and AKT signaling in CML cells^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

517.06

C₃₁H₃₃ClN₂O₃

618430-39-0

O=C1C(CC2=CC=CC=C2)=C([[email protected]@H](C(C)C)N(C(C3=CC=C(C)C=C3)=O)CCCN)OC4=CC(Cl)=CC=C41

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]