An Eg5 inhibitor
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SB-743921 (hydrochloride)

Item No. 18384

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-aminopropyl)-N-[(1R)-1-[7-chloro-4-oxo-3-(phenylmethyl)-4H-1-benzopyran-2-yl]-2-methylpropyl]-4-methyl-benzamide, monohydrochloride
CAS Number
940929-33-9
Molecular Formula
C31H33ClN2O3 • HCl
Formula Weight
553.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMSO: 50 mg/mlEthanol: 20 mg/mlPBS (pH 7.2): 0.2 mg/ml
λmax
203, 309 nm
SMILES
ClC1=CC=C(C(C(CC2=CC=CC=C2)=C([C@H](N(C(C3=CC=C(C)C=C3)=O)CCCN)C(C)C)O4)=O)C4=C1.Cl
InChi Code
InChI=1S/C31H33ClN2O3.ClH/c1-20(2)28(34(17-7-16-33)31(36)23-12-10-21(3)11-13-23)30-26(18-22-8-5-4-6-9-22)29(35)25-15-14-24(32)19-27(25)37-30;/h4-6,8-15,19-20,28H,7,16-18,33H2,1-3H3;1H/t28-;/m1./s1
InChi Key
MLMZVWABFOLFGV-LNLSOMNWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Cayman Chemical
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    Product Description

    SB-743921 is a potent inhibitor of the kinesin spindle protein Eg5 (Ki = 0.5 nM for microtubule-stimulated ATPase activity).1 It inhibits the growth of HCT116 colon, LNCaP and PC3 prostate, K562 leukemia, BxPC-3 pancreas, and NCI-H1299 lung cancer cell lines in vitro (GI50s = 25, 22, 48, 50, 80, and 82 nM, respectively). In vivo, SB-743921 induces complete tumor regression in a COLO 205 mouse xenograft model and partial regression in MCF-7, SK-MES, H69, and OVCAR-3 mouse xenograft models.2 SB-743921 (2.5-10 mg/kg) also reduces tumor volume in a dose-dependent manner in a diffuse large B cell lymphoma (DLBCL) mouse xenograft model.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Good, J.A.D., Wang, F., Rath, O., et al. 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(5), 1878-1893 (2015).

    2. Jackson, J.R., Gilmartin, A., Dhanak, D., et al. Abstract B11: A second generation KSP inhibitor, SB-743921, is a highly potent and active therapeutic in preclinical models of cancer. Clin. Cancer Res. 12(19 Suppl), (2006).

    3. Bongero, D., Paoluzzi, L., Marchi, E., et al. The novel kinesin spindle protein (KSP) inhibitor SB-743921 exhibits marked activity in in vivo and in vitro models of aggressive large B-cell lymphoma. Leuk. Lymphoma 56(10), 2945-2952 (2015).