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SB-743921

Chemical Structure : SB-743921

CAS No.: 940929-33-9

SB-743921 (SB743921;SB 743921)

Catalog No.: PC-42882Not For Human Use, Lab Use Only.

SB-743921 is a potent, selective kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, shows no activity against MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SB-743921 is a potent, selective kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, shows no activity against MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E; also shows high affinity for mouse KSP with Ki of 0.12 nM; blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death in cancer cells, demonstrates improved potency over ispinesib in both biochemical and cellular assays; shows a broad spectrum of tumor inhibition in multiple cancer models.

Blood Cancer

Phase 2 Discontinued

Physicochemical Properties

M.Wt 553.5193
Formula C31H34Cl2N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzamide, N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methyl-, hydrochloride (1:1)

References

1. Good JA, et al. J Med Chem. 2013 Mar 14;56(5):1878-93.

2. Holen KD, et al. Cancer Chemother Pharmacol. 2011 Feb;67(2):447-54.

3. Zhu L, et al. Anticancer Drugs. 2016 Oct;27(9):863-72.

4. Talapatra SK, et al. J Med Chem. 2013 Aug 22;56(16):6317-29.

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