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ISPINESIB | ISPINESIB : Inhibitor of KIF11
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
KIF11
  • Ki:1.7 ± 0.1 nM
  • GI50:45 nM
  • GI50:19 nM
Inhibitor
150 nM, up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
At 20 µM inhibitor concentration, more than 10000-fold the Ki for KSP, no inhibitory activity was ob ...

Potency
Cellular
In Vitro

KIF11

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/bi702061g

In Vivo Validations

Mouse
Dose:
Route of delivery: Oral
Cmax: 0.3 ug/ mL
Tmax: 2.7 h
Area Under the Curve:: 1.5 ug*h/mL
Bioavailability: 45%

DOI Reference: 10.1021/jm3014597

Dose:
Route of delivery: Intravenous
Plasma half life: 4.1 h
Systemic clearance: 20.5 mL/min/kg
Area Under the Curve:: 3.1 ug*h/mL
Volume of Distribution at Steady-State: 2.5 L/Kg

DOI Reference: 10.1021/jm3014597

Chemical Information

Molecular Formula C30H33ClN4O2
SMILEs Cc1ccc(C(=O)N(CCCN)[C@@H](c2nc3cc(Cl)ccc3c(=O)n2Cc2ccccc2)C(C)C)cc1
InChI InChI=1S/C30H33ClN4O2/c1-20(2)27(34(17-7-16-32)29(36)23-12-10-21(3)11-13-23)28-33-26-18-24(31)14-15-25(26)30(37)35(28)19-22-8-5-4-6-9-22/h4-6,8-15,18,20,27H,7,16-17,19,32H2,1-3H3/t27-/m1/s1
Molecular weight 516.23 Da
AlogP 5.59492
HBond acceptors 6
HBond donors 2
Atoms 70

Vendors

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Expert Reviews

No SERP comments found for ISPINESIB

Probe ISPINESIB is in the process of SERP review.

Please continue to check back for new reviews and commentary.