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Submit ReviewSB 743921 hydrochloride is a potent kinesin spindle protein (KSP) inhibitor (Ki = 0.1 nM). Induces cell mitotic arrest and apoptosis in vitro. Inhibits the growth of a range of tumor cells in vitro, including colon (HCT 116), prostate (PC-3) and leukemia (K-562) cancer cell lines. Causes tumor regression in human tumor xenograft models in vivo, including colon (Colo205), lung (H69) and breast (MCF7) cancer cell xenografts.
Sold with the permission of GlaxoSmithKline.
分子量 | 553.52 |
公式 | C31H33ClN2O3.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 940929-33-9 |
PubChem ID | 49867937 |
InChI Key | MLMZVWABFOLFGV-LNLSOMNWSA-N |
Smiles | ClC1=CC=C2C(OC([C@@H]([C@H](C)C)N(C(C4=CC=C(C)C=C4)=O)CCCN)=C(CC3=CC=CC=C3)C2=O)=C1.Cl |
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Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Jackson et al (2006) 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 and Diagnostics in Cancer Therapeutic Development. Abstract (B11)
Good et al (2013) 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. 56 1878 PMID: 23394180
Talapatra et al (2013) Mitotic kinesin Eg5 overcomes inhibition to the phase I/II clinical candidate SB743921 by an allosteric resistance mechanism. J.Med.Chem. 56 6317 PMID: 23875972
关键词: SB 743921 hydrochloride, SB 743921 hydrochloride supplier, SB743921, hydrochloride, potent, kinesin, spindle, protein, inhibitors, inhibits, KSP, EG5, antitumor, apoptosis, Kinesin, 5109, Tocris Bioscience
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