2244992-76-3
2244992-76-3 structure
- Name: CHMFL-PI3KD-317
- Chemical Name: CHMFL-PI3KD-317
- CAS Number: 2244992-76-3
- Molecular Formula: C21H24ClN5O3S2
- Molecular Weight: 494.03
- Catalog: Signaling Pathways PI3K/Akt/mTOR PI3K
- Create Date: 2019-03-03 14:34:59
- Modify Date: 2024-01-13 17:33:41
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CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50s of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells[1].
| Name | CHMFL-PI3KD-317 |
|---|---|
| Synonyms | MFCD31813683 |
| Description | CHMFL-PI3KD-317 is a highly potent, selective and orally active PI3Kδ inhibitor, with an IC50s of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM. CHMFL-PI3KD-317 has antiproliferative effects on cancer cells[1]. |
|---|---|
| Related Catalog | |
| Target |
PI3Kδ:6 nM (IC50) PI3Kα:62.6 nM (IC50) PI3Kβ:284 nM (IC50) PI3Kγ:202.7 nM (IC50) PIK3C2B:882.3 nM (IC50) Vps34:1801.7 nM (IC50) PI4KIIIA:574.1 nM (IC50) PI4KIIIB:300.2 nM (IC50) |
| In Vitro | CHMFL-PI3KD-317 (Compound 15i) is a highly potent and selective PI3Kδ inhibitor, with an IC50s of 6 nM, and exhibits over 10-1500 fold selectivity over other class I, II and III PIKK family isoforms, such as PI3Kα (IC50, 62.6 nM), PI3Kβ (IC50, 284 nM), PI3Kγ (IC50, 202.7 nM), PIK3C2A (IC50, >10000 nM), PIK3C2B (IC50, 882.3 nM), VPS34 (IC50, 1801.7 nM), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM)[1]. In cellular assay, CHMFL-PI3KD-317 inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells, with an EC50 of 4.3 nM[1]. CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 3.5 ± 0.8, 4.0 ± 0.9, 4.8 ± 0.2, 3.3 ± 0.2, 3.0 ± 0.4 μM against PF382, NALM-6, MV4-11, MOLM-14 and MOLM-13 cells, respectively[1]. |
| In Vivo | CHMFL-PI3KD-317 (Compound 15i) shows favorable oral bioavailability and acceptable half-life (T1/2 = 3.28 h) in Sprague-Dawley rats[1]. CHMFL-PI3KD-317 (25, 50 and 100 mg/kg/day, p.o.) inhibits the growth of the MOLM14 tumor in mice[1]. |
| References |
| Molecular Formula | C21H24ClN5O3S2 |
|---|---|
| Molecular Weight | 494.03 |
| Storage condition | -20°C |