SB 743921 hydrochloride

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Cat.No. 5109 - SB 743921 hydrochloride | C31H33ClN2O3.HCl | CAS No. 940929-33-9
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
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Literature

Biological Activity

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.

Compound Libraries

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 553.52. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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References

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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