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PIM-447 | Inhibitor of PIM1, PIM2, PIM3
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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
PIM1
  • Ki:0.006 nM
  • EC50:170 nM
PIM2
  • Ki:0.018 nM
  • EC50:170 nM
PIM3
  • Ki:0.009 nM
  • EC50:170 nM
Inhibitor
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Kinase selectivity was first determined in biochemical assays for a panel of 68 protein kinases and ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Cellular activity across an expanded panel of 26 AML cell lines was assessed with antiproliferative ...

Potency
Cellular
In Vitro

PIM1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5b01275

PIM2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.5b01275

PIM3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.5b01275

In Vivo Validations

Mouse, Rat, Dog
Dose: 30 or 100 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 3.3 (M), 2.8 (R), 6.7 (D) h
Systemic clearance: 20 (M), 28 (R), 8 (D) mL/min/Kg

DOI Reference: 10.1021/acs.jmedchem.5b01275

Negative Control Compounds

cpd 1

Orthogonal Probes def

SGI-1776
AZD-1208

Chemical Information

Molecular Formula C24H23F3N4O
SMILEs C[C@@H]1C[C@H](N)C[C@H](c2ccncc2NC(=O)c2ccc(F)c(-c3c(F)cccc3F)n2)C1
InChI InChI=1S/C24H23F3N4O/c1-13-9-14(11-15(28)10-13)16-7-8-29-12-21(16)31-24(32)20-6-5-19(27)23(30-20)22-17(25)3-2-4-18(22)26/h2-8,12-15H,9-11,28H2,1H3,(H,31,32)/t13-,14+,15-/m0/s1
Molecular weight 440.18 Da
AlogP 0.0
HBond acceptors 5
HBond donors 3
Atoms 55

References

Publications

Cross References

canSARChEMBLBindingDBPDBPubMed

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 10 Apr 2021 )
Cellular Use Rating
In Model Organisms
PIM-447 is a pan-PIM 1, 2 and 3 kinase inhibitor that demonstrates potent biochemical activity and good selectivity in a 442 kinase panel. There is a large drop off to cellular activity in both antiproliferative...
by SERP
(on 10 Apr 2021 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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