SB743921 Inhibitor CAS No. 940929-33-9

Cat. No.	Name	Size	Price
KI2707	SB743921	5 mg	$272
	SB743921	10 mg	$512
	SB743921	25 mg	$820
	SB743921	50 mg	$1552
	SB743921	100 mg	$2482
	SB743921	200 mg	$3952

Chemical Characteristic

Product Name	SB743921
CAS No.	940929-33-9
Molecular Weight	553.53
Formula	C₃₁H₃₄Cl₂N₂O₃
Chemical Name	N-(3-aminopropyl)-N-[(1R)-1-(3-benzyl-7-chloro-4-oxochromen-2-yl)-2-methylpropyl]-4-methylbenzamide;hydrochloride
Smiles	C(=O)(c1ccc(cc1)C)N(C(C(C)C)c1c(c(=O)c2ccc(cc2o1)Cl)Cc1ccccc1)CCCN Cl
Chemical Structure

Biological activities

SB743921 is a second generation kinesin spindle protein (KSP) inhibitor. SB743921 inhibits KSP (Eg5) with a Ki of 0.1 nM. SB-743921 inhibits SKOV3, Colo205, MV522, MX1 with IC50s of 0.2, 0.07, 1.7, 0.06 nM, respectively.^[1] SB743921 disrupts assembly of functional bipolar mitotic spindles causing cell cycle arrest in mitosis and subsequent cell death in diffuse large B-Cell lymphoma lines. SB743921 exhibits potent cytotoxicity in diffuse large B-Cell lymphoma lines, with IC50s ranging from 0.13 to 627 nM. In vitro, SB743921 shows cytotoxicity in DLBCL pulse chase exposure, with IC50s ranging from 22.58 nM to 627 nM.^[2] In vivo, SB743921 has an impressive spectrum of activity in tumor models, such as advanced human tumor xenografts Colo205 (complete regressions), MCF-7, SK-MES, H69, OVCAR-3 (complete and partial regressions), HT-29, MX-1, MDA-MB-231, A2780 (tumor growth delay). In female BDF1 mice, SB743921 shows great efficacy against P388 lymphocytic leukemia. SB743921 also causes complete regression of advanced sc human Colo205 colon carcinoma xenografts in B6D2F1 Mice.^[1]

Protocols

In vitro, SB-743921 is dissolved in DMSO.^[1]

References

[1] Jackson JR, et al. 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 Diagnostics in Cancer Therapeutic Development. 2006. [2] Zain D, et al. Translational development of the novel kinesin spindle protein (KSP/Eg5) inhibitor SB-743921 (SB-921) in lymphoma: from preclinical models to phase 1 studies. 2008.

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