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XL019 | Inhibitor of JAK2
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

Targets Biochemical/Biophysical Potency Cellular Potency
JAK2
  • IC50:2.2 nM JAK2; 214 nM JAK3; 134 nM JAK1
  • IC50:386.4 nM pSTAT1; 695 nM pSTAT3
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Evaluated against a selectivity panel of 118 kinases. displaying >50-fold selectivity against ...

Potency
Cellular
In Vitro

JAK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

In Vivo Validations

Mouse, Rat, Dog, Cyno
Dose: 30-300 mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 1.94 (M), 3.23 (R), 5.06 (D), 3.36 (C) h PO
Systemic clearance: 4951.7(M), 129.2(R), 1397.5(D), 1174.7(C) mg/h/Kg

Reference: --

Orthogonal Probes def

Gandotinib
BMS-911543
AZ-960

Chemical Information

Molecular Formula C25H28N6O2
SMILEs O=C(Nc1ccc(-c2ccnc(Nc3ccc(N4CCOCC4)cc3)n2)cc1)[C@H]1CCCN1
InChI InChI=1S/C25H28N6O2/c32-24(23-2-1-12-26-23)28-19-5-3-18(4-6-19)22-11-13-27-25(30-22)29-20-7-9-21(10-8-20)31-14-16-33-17-15-31/h3-11,13,23,26H,1-2,12,14-17H2,(H,28,32)(H,27,29,30)/t23-/m1/s1
Molecular weight 444.23 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 61
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

    Cross References

    canSARChEMBLBindingDBPDB

    Vendors

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

    Expert Reviews

    by SERP
    (on 26 Feb 2021 )
    Cellular Use Rating
    In Model Organisms
    Forsyth and coworkers present in the given reference the development of an aminopyrimidine based JAK2 inhibitor. Comprehensive SAR and characterization via enzymatic and cellular assays is given throughout...
    by SERP
    (on 12 Mar 2021 )
    Cellular Use Rating
    In Model Organisms
    Compound XL019 (CPP1230, O19, cpd 10d) appears to be a good tool molecule for JAK2 that can be used both in cellular and in vivo studies. The compound shows single-digit nM activity against JAK2 biochemically,...
    by SERP
    (on 13 Mar 2021 )
    Cellular Use Rating
    In Model Organisms
    This is a potent inhibitor of JAK2 with selectivity against JAK1/JAK3 and other kinases and good probe properties for interrogating the target in vitro and in vivo. Data on broad kinome selectivity...
    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