1911564-39-0
1911564-39-0 structure
- Name: PI3Kδ-IN-1
- Chemical Name: PI3Kδ-IN-1
- CAS Number: 1911564-39-0
- Molecular Formula: C22H20F3N7O2
- Molecular Weight: 471.44
- Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
- Create Date: 2019-03-30 16:06:34
- Modify Date: 2024-01-06 00:43:24
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PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM.
| Name | PI3Kδ-IN-1 |
|---|
| Description | PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 1.7 nM (PI3Kδ)[1] |
| In Vitro | PI3Kδ-IN-1 (compound 52) shows >100-fold selectivity over the other PI3K isoforms. Kinome selectivity is also excellent with >660-fold selectivity over MNK1 and others in HTRF assays. Importantly, PI3Kδ-IN-1 has an improved human/rodent in vitro stability correlation and a good permeability profile[1]. |
| In Vivo | PI3Kδ-IN-1 (2, 5 mg/kg, orally b.i.d. for 42 days) shows greater than 50% suppression of paw swelling in mice. PI3Kδ-IN-1 has an EC50 of 10 nM at 24 h (ED50 of ∼1.25 mg/kg) in mice[1]. Animal Model: Male DBA/1 mice (20−25g)[1] Dosage: 0.5, 2, 5 mg/kg Administration: Oral b.i.d. for 42 days, Result: A dose dependent reduction of the clinical score was observed. Doses of 2 and 5 mg/kg showed greater than 50% suppression of paw swelling[1]. |
| References |
| Molecular Formula | C22H20F3N7O2 |
|---|---|
| Molecular Weight | 471.44 |