Chemical Probes logo
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
Download

Probe Summary

More...

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
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

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 5.044100000000004
HBond acceptors 5
HBond donors 3
Atoms 55

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 public comments)
If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria