2. Cell Cycle/DNA Damage
    Cytoskeleton
  3. Kinesin
  4. SB-743921 hydrochloride

SB-743921 hydrochloride 

Cat. No.: HY-12069 Purity: 98.00%
COA Handling Instructions

SB-743921 hydrochloride 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 hydrochloride Chemical Structure

SB-743921 hydrochloride Chemical Structure

CAS No. : 940929-33-9

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 161 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 161 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 226 In-stock
Estimated Time of Arrival: December 31
50 mg USD 710 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1045 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of SB-743921 hydrochloride:

Top Publications Citing Use of Products

2 Publications Citing Use of MCE SB-743921 hydrochloride

View All Kinesin Isoform Specific Products:

View All Isoforms
Kinesin-5/Eg5/KSP Kinesin-6 Kinesin-7/CENP-E Kinesin-12 Kinesin-14

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

SB-743921 hydrochloride 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

553.52

Appearance

Solid

Formula

C31H34Cl2N2O3
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (180.66 mM)

H2O : 10 mg/mL (18.07 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.52 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
Cell Assay
[2]

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]

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SB-743921940929-33-9SB743921SB 743921KinesinInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
SB-743921 hydrochloride
Cat. No.:
HY-12069
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email address *

Phone number

 

Department *

Organization name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.