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SB 743921 hydrochloride

Cat. No. 5109 Submit a Review Datasheet / COA / SDS
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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)
Datasheet
Citations
Reviews
Literature (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

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.

Solubility Data for SB 743921 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.35 100

Preparing Stock Solutions for SB 743921 hydrochloride

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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

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Product Datasheets for SB 743921 hydrochloride

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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

If you know of a relevant reference for SB 743921 hydrochloride, please let us know.

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Citations for SB 743921 hydrochloride

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Literature in this Area

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Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

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