1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Kinesin

SB-743921 

Cat. No.: HY-12069 Purity: 97.31%
Handling Instructions

SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.

For research use only. We do not sell to patients.

SB-743921 Chemical Structure

SB-743921 Chemical Structure

CAS No. : 940929-33-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 290 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 815 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.

IC50 & Target[1]

Eg5

0.1 nM (Ki)

In Vitro

SB-743921 is a potent inhibitor of Eg5, with a Ki of 0.1 nM[1]. SB-743921 (1 nM) potently inhibits colony forming cell (CFC) formation of chronic myeloid leukemia (CML) primary cells, but exhibits slight inhibitory activities on the colony-forming ability of normal bone marrow progenitors. SB-743921 (1, 3 nM) induces apoptosis of CML primary CD34 + cells, and shows slight effect on normal CD34 + cells. SB-743921 (2 nM) in combination with imatinib displays additive anti-proliferative effect in KCL22 and CML CD34 + cells. Furthermore, SB-743921 overcomes imatinib resistance in CML cells. SB-743921 (0.5 nM, 1 nM, 3 nM) inhibits MEK/ERK and AKT signaling in CML cells[2].

In Vivo

SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts[3].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.8066 mL 9.0331 mL 18.0662 mL
5 mM 0.3613 mL 1.8066 mL 3.6132 mL
10 mM 0.1807 mL 0.9033 mL 1.8066 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

SB-743921 is dissolved in DMSO.

K562 and KCL22 cells are seeded in six-well plates at a number of 5 × 105 in 2 mL RPMI-1640 medium supplemented with 10% FBS in a 5% CO2 atmosphere at 37°C, and are treated with control (2% DMSO), 50 nM imatinib, 2 nM SB-743921 and 50 nM imatinib + 2 nM SB-743921, respectively. Cell number and viability are determined every 24 h. Results are plotted for live cells against time to generate a growth curve[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

SB-743921 is formulated in 8% DMSO, 2% Tween 80, distilled water (pH 5).

The animal experiments are performed with female NMRI nu/nu mice. Tumor fragments are obtained from xenografts in serial passage in nude mice. Mice are randomized to the various groups, and dosing is started when the required number of mice carries a tumor of 50-250 mm3 volume, preferably 80-200 mm3. Vehicle for 1: 10% ethanol, 10% cremophor, 80% D5W (dextrose 5%); vehicle for all other compounds (including SB-743921): 8% DMSO, 2% Tween 80, distilled water (pH 5). All treatments are given intraperitoneally. Vehicle control mice (group 1) are treated with 10 mL/kg vehicle on days 0, 3, 6, 8, 10, 13, 20, 22, 24, 29, 31, 34, 36, 38, 48, 51, 55, 58, 62, 65, and 69[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

553.52

Formula

C₃₁H₃₄Cl₂N₂O₃

CAS No.

940929-33-9

SMILES

ClC1=CC2=C(C(C(CC3=CC=CC=C3)=C([[email protected]@H](C(C)C)N(C(C4=CC=C(C=C4)C)=O)CCCN)O2)=O)C=C1.Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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SB-743921
Cat. No.:
HY-12069
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