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AZD-6482 | ATP competitive of PIK3CB
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
PIK3CB
  • IC50:0.69 nM
  • IC50:100-500 nM
ATP competitive
0.1 – 0.5 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - PI3Ka 136 nM, PI3Kd 13.6 nM, PI3Kg 47.8 nM, DNA-PK 53.7 nM, PI3K-C2b 54.1 nM

Potency Assay Off-Target:
In Vitro kinase assay measurements against recombinant PI3Ks and PIKK using SelectScreen (Invitrogen ...
Selectivity Assessment Description:
In Vitro kinase assay showed that AZD-6482 has 200-, 20-, and 70-fold selectivity over p110α, p11 ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Tested cell proliferation on a large panel of 422 cancer cell lines using high-throughput tumor c ...

Potency
Cellular
In Vitro

PIK3CB

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/2159-8290.CD-12-0003

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Oral
Plasma half life: 2.75 h
Systemic clearance: 148 mL/min/Kg
Cmax: 780 ng/mL
Area Under the Curve:: 112 h*ng/mL
Volume of Distribution at Steady-State: 10.3 L/Kg

DOI Reference: 10.1158/2159-8290.CD-12-0003

Dose: 10 mg/Kg
Route of delivery: Oral
Cmax: 74.1 ng/mL
Tmax: 0.25 h
Area Under the Curve:: 101 h*ng/mL
Bioavailability: 6.85%

DOI Reference: 10.1158/2159-8290.CD-12-0003

Dose: 10 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 1.1 h
Cmax: 2074 ng/mL
Tmax: 0.08 h
Area Under the Curve:: 1140 h*ng/mL

DOI Reference: 10.1158/2159-8290.CD-12-0003

Chemical Information

Molecular Formula C22H24N4O4
SMILEs Cc1cc([C@@H](C)Nc2ccccc2C(=O)O)c2nc(N3CCOCC3)cc(=O)n2c1
InChI InChI=1S/C22H24N4O4/c1-14-11-17(15(2)23-18-6-4-3-5-16(18)22(28)29)21-24-19(12-20(27)26(21)13-14)25-7-9-30-10-8-25/h3-6,11-13,15,23H,7-10H2,1-2H3,(H,28,29)/t15-/m1/s1
Molecular weight 408.18 Da
AlogP 2.710820000000001
HBond acceptors 8
HBond donors 2
Atoms 54

Vendors

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Expert Reviews

by SERP
(on 23 Nov 2020)
Cellular Use Rating
In Model Organisms
Given that the profiling data available at this point uses an in vitro affinity binding assay that does not use ATP, it is difficult to assess the intracellular selectivity profile (which may very well...
by SERP
(on 8 Dec 2020)
Cellular Use Rating
In Model Organisms
AZ6482 is a highly selective and potent chemical probe for PI3Kbeta. It is suitable for study the role of the target in model cell systems and animal studies.
by SERP
(on 18 Dec 2020)
Cellular Use Rating
In Model Organisms
AZD-6482 is a suitable chemical probe for assessing PIK3CB (PI3Kbeta) function. The compound is 8-fold selective over PI3Kdelta in in vitro assays and so care should be taken when used in cellular studies...
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