IOA-244 |
IOA-244 : non-ATP competitive inhibitor of PIK3CD
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| PIK3CD |
|
|
non-ATP competitive
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity in Jurkat cell lysate was measured using the KiNativ method at 10 uM.
Selectivity Assessment Description:
Selective against Isoforms: IC50 PI3Kα 10.1 μM, IC50 PI3Kβ 0.43 μM, IC50 PI3Kγ >15 μM
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The same KiNativ platform was also used to measure the potency and selectivity of IOA-244 in human w ...
Potency Cellular
In Vitro
PIK3CD
Mode of Action: non-ATP competitive
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1158/2767-9764.CRC-22-0477
In Vivo Validations
Mouse
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.33 h
Systemic clearance:
1.43 L/h/Kg
Volume of Distribution at Steady-State:
1.81 L/Kg
DOI Reference: 10.1158/2767-9764.CRC-22-0477
Dose: 5 mg/Kg
Route of delivery:
Oral
Bioavailability:
73%
DOI Reference: 10.1158/2767-9764.CRC-22-0477
Dose: 30 mg/Kg
Route of delivery:
Oral
Cmax:
6647 ng/mL
Area Under the Curve::
13480 h×ng/mL
DOI Reference: 10.1158/2767-9764.CRC-22-0477
Rat
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
4.82 h
Systemic clearance:
0.427 L/h/Kg
Volume of Distribution at Steady-State:
2.32 L/Kg
DOI Reference: 10.1158/2767-9764.CRC-22-0477
Dose: 5 mg/Kg
Route of delivery:
Oral
Bioavailability:
105%
DOI Reference: 10.1158/2767-9764.CRC-22-0477
Dose: 30 mg/Kg
Route of delivery:
Oral
Cmax:
8505 ng/mL
Area Under the Curve::
57150 h*ng/mL
DOI Reference: 10.1158/2767-9764.CRC-22-0477
Chemical Information
| Molecular Formula | C26H27FN4O5S |
| InChI | InChI=1S/C26H27FN4O5S/c27-22-3-1-2-20-24-21(17-37(33,34)25(20)22)23(26(32)30-10-14-36-15-11-30)28-31(24)19-6-4-18(5-7-19)16-29-8-12-35-13-9-29/h1-7H,8-17H2 |
| Molecular weight | 526.17 Da |
| AlogP | 0.0 |
| HBond acceptors | 9 |
| HBond donors | -- |
| Atoms | 64 |