SB 743921 hydrochloride

Discontinued Product

5109 has been discontinued.

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说明: Potent kinesin spindle protein (KSP) inhibitor
化学名: N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methylbenzamide hydrochloride
纯度: ≥98% (HPLC)
说明书
引用文献
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文献 (1)

生物活性 for SB 743921 hydrochloride

SB 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.

许可信息

Sold with the permission of GlaxoSmithKline.

技术数据 for SB 743921 hydrochloride

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.

产品说明书 for SB 743921 hydrochloride

参考文献 for SB 743921 hydrochloride

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

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