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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.
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| 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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 55.35 | 100 |
以下数据基于产品分子量 553.52。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.81 mL | 9.03 mL | 18.07 mL |
| 5 mM | 0.36 mL | 1.81 mL | 3.61 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.81 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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
If you know of a relevant reference for SB 743921 hydrochloride, please let us know.
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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