SB-743921 free base

CAS: 618430-39-0 F: C31H33ClN2O3 W: 517.06

SB-743921 free base is a potent selective inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM. SB-743921 fre

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Bioactivity	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].
Invitro	SB-743921 是一种有效的 Eg5 抑制剂，Ki 为 0.1 nM[1]。 SB-743921 (1 nM) 有效抑制慢性粒细胞白血病 (CML) 原代细胞的集落形成细胞 (CFC) 形成，但对正常骨髓祖细胞的集落形成能力表现出轻微的抑制活性[2]。 SB-743921 (1-3 nM) 诱导 CML 原代 CD34+ 细胞凋亡，对正常 CD34+ 细胞有轻微影响。 SB-743921 与伊马替尼联合使用，在 KCL22 和 CML CD34+ 细胞中表现出附加的抗增殖作用。此外，SB-743921 克服了 CML 细胞对伊马替尼的耐药性[2]。 SB-743921（0.5 nM、1 nM、3 nM）抑制 CML 细胞中的 MEK/ERK 和 AKT 信号传导[2]。
In Vivo	SB-743921 具有良好的口服生物利用度和药代动力学，可诱导携带肺癌患者异种移植物的裸鼠肿瘤完全消退[3]。
Name	SB-743921 free base
CAS	618430-39-0
Formula	C31H33ClN2O3
Molar Mass	517.06
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.