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PRT062607 | Inhibitor of SYK
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
SYK
  • IC50:6.0 ± 0.2 nM
  • IC50:2.1 ± 0.4 nM
  • IC50:160 - 400 nM
  • IC50:120 ± 5 nM
Inhibitor
100 nM - 2 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - FGR 81 nM, MLK1 88 nM, YES 123 nM, FLT3 139 nM, PAK5 166 nM, LYN 192 nM, SRC 244 nM, LCK 249 nM, PYK2 108 nM

Potency Assay Off-Target:
Radiometric assay. At 50 nM, P505-15 was selective for SYK over 270 other kinases; at 300 nM, it inh ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
No activity was detected against LYN substrates in B cells.

Potency
Cellular
In Vitro

SYK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1124/jpet.111.188441

In Vivo Validations

Mouse
Dose: 10, 15, 20 mg/kg BID
Route of delivery: Oral
Cmax: 466, 893, 1484 nM
Tmax: 1.5 - 4.0 h
Area Under the Curve:: 738, 1671, 3191 ng*h/ml

PMID Reference: 23220742

Orthogonal Probes def

ENTOSPLETINIB

Chemical Information

Molecular Formula C19H23N9O
SMILEs NC(=O)c1cnc(N[C@@H]2CCCC[C@@H]2N)nc1Nc1cccc(-n2nccn2)c1
InChI InChI=1S/C19H23N9O/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27)/t15-,16+/m0/s1
Molecular weight 393.20 Da
AlogP 1.5815999999999988
HBond acceptors 10
HBond donors 6
Atoms 52

Vendors

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Expert Reviews

by SERP
(on 6 May 2016)
Cellular Use Rating
In Model Organisms
I recommend this compound as "best available" for use in cells; it is potent and cell active and almost meets a high bar for selectivity when broadly profiled. I also recommend this compound as "best...
by SERP
(on 10 Sept 2016)
Cellular Use Rating
In Model Organisms
P505-15 is a small molecule, and a potent and selective inhibitor of SYK. It inhibits SYK and suppresses BCR signaling in SUDHL4 cells and inhibits SYK-dependent signaling in human whole blood. P505-15...
by SERP
(on 28 Apr 2017)
Cellular Use Rating
In Model Organisms
Highly selective inhibitor of Spleen Tyrosine Kinase (SYK). Exhibits ~80-fold selectivity for SYK over the next target. Shows 1 nM potency against SYK, with substantially lower potency towards the three...
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