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Chemical Structure| 940929-33-9 Chemical Structure| 940929-33-9

Structure of SB-743921 HCl
CAS No.: 940929-33-9

Chemical Structure| 940929-33-9

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SB-743921 is a potent KIF11 inhibitor with Ki value of 0.1 nM.

Synonyms: SB-743921; SB-743921 (hydrochloride); SB-743921 hydrochloride

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Product Details of SB-743921 HCl

CAS No. :940929-33-9
Formula : C31H34Cl2N2O3
M.W : 553.52
SMILES Code : O=C(N(CCCN)[C@@H](C1=C(CC2=CC=CC=C2)C(C3=C(O1)C=C(Cl)C=C3)=O)C(C)C)C4=CC=C(C)C=C4.[H]Cl
Synonyms :
SB-743921; SB-743921 (hydrochloride); SB-743921 hydrochloride
MDL No. :MFCD18385010
InChI Key :MLMZVWABFOLFGV-LNLSOMNWSA-N
Pubchem ID :49867937

Safety of SB-743921 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of SB-743921 HCl

cytoskeleton

Isoform Comparison

Biological Activity

Target
  • Kinesin

    KSP (P388 cells), IC50:14.4 nM

    KSP, Ki:0.07 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Cryptosporidium parvum sporozoites 100 µM 1 hour SB-743921 completely inhibited the secretion of CpTSP4 PMC10865969
CHLA-10 1.0 nM 24 hours To evaluate the effect of SB-743921 combined with VIC-1911 on cell cycle, the results showed that the combination treatment significantly increased the proportion of cells in the G2/M phase. PMC10605681
HeLa cells 1.25 nM 3 hours To study the effect of SB743921 on spindle formation in HeLa cells, results showed that 1.25 nM did not increase the frequency of monoastral mitosis PMC5528592
HeLa cells 10 nM 48 hours To study the effect of SB743921 on HeLa cell proliferation, results showed no significant effect on cell proliferation at concentrations up to 1.25 nM PMC5528592
HSC4 cells 0, 0.1, 1.0, 10 nM 48 hours To evaluate the effect of SB-743921 on the cell cycle of HSC4 cells, the results showed that SB-743921 treatment significantly increased the proportion of cells in sub-G1 and G2/M phases. PMC5743338
TC-71 0.625 nM 7 days To evaluate the effect of SB-743921 combined with VIC-1911 on EWS cell survival, the results showed that the combination treatment significantly reduced colony formation. PMC10605681
SK-ES-1 0.625 nM 7 days To evaluate the effect of SB-743921 combined with VIC-1911 on EWS cell survival, the results showed that the combination treatment significantly reduced colony formation. PMC10605681
HSC4 cells 0, 0.1, 1.0, 10 nM 72 hours To evaluate the effect of SB-743921 on the growth of HSC4 cells, the results showed that SB-743921 significantly decreased cell viability in a dose-dependent manner. PMC5743338

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice EWS xenograft model Intraperitoneal injection 1.25 mg/kg 3 times a week for 6 weeks To evaluate the efficacy of SB-743921 combined with VIC-1911 in the EWS xenograft model, the results showed that the combination treatment significantly delayed tumor growth and improved overall survival. PMC10605681

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00136513 Solid Tumor Cancer PHASE1 COMPLETED - GSK Investigational Site, Pitt... More >>sburgh, Pennsylvania, 15232, United States|GSK Investigational Site, Madison, Wisconsin, 53792, United States Less <<
NCT00343564 Non-Hodgkin's Lymphoma ... More >> Hodgkin's Disease Less << Phase 1 Phase 2 Completed - United States, New Jersey ... More >> Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 United States, New York Cornell University Medical Center New York, New York, United States, 10021 Memorial Sloan-Kettering Caner Center New York, New York, United States, 10021 Herbert Irving Comprehensive Cancer Center New York, New York, United States, 10032 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Tennessee Sarah Cannon Cancer Research Institute Nashville, Tennessee, United States, 37203 Russian Federation Russian Medical Academy of Postgraduate Education Moscow, Russian Federation, 115478 St. Petersburg State PAVLOV Medical University Saint Petersburg, Russian Federation, 197002 Less <<
NCT00343564 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.03mL

1.81mL

0.90mL

18.07mL

3.61mL

1.81mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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