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Submit ReviewSB 743921 hydrochloride
Description: Potent kinesin spindle protein (KSP) inhibitor
Chemical Name: N-(3-Aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methylbenzamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity 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.
Licensing Information
Sold with the permission of GlaxoSmithKline.
Technical Data for SB 743921 hydrochloride
| M. Wt | 553.52 |
| Formula | C31H33ClN2O3.HCl |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for SB 743921 hydrochloride
References for SB 743921 hydrochloride
References are publications that support the biological activity of the product.
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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Cell Cycle and DNA Damage Research Product Guide
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