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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $93 | In Stock | |
5 mg | $228 | In Stock | |
10 mg | $347 | In Stock | |
25 mg | $625 | In Stock | |
50 mg | $939 | In Stock | |
100 mg | $1,280 | In Stock | |
1 mL x 10 mM (in DMSO) | $248 | In Stock |
Description | CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3Kδ inhibitor with an IC50 of 6 nM, exhibiting 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). It inhibits PI3Kδ-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells. |
Targets&IC50 | PI4KIIIB:300.2 nM, PI3Kδ:6 nM, PI3Kγ:202.7 nM, PI3Kα:62.6 nM, VPS34:1801.7 nM, PI4KIIIA:574.1 nM, PI3Kβ:284 nM, PIK3C2B:882.3 nM |
In vitro | CHMFL-PI3KD-317 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), PI4KIIIA (IC50, 574.1 nM) and PI4KIIIB (IC50, 300.2 nM). CHMFL-PI3KD-317 has antiproliferative effects, with GI50s of 4.0, 3.5, 4.8, 3.0, 3.3 μM against NALM-6, PF382, MV4-11, MOLM-13 cells, and MOLM-14, respectively. |
In vivo | CHMFL-PI3KD-317 (Compound 15i; 25, 50, and 100 mg/kg/day, p.o., for 14 days) inhibits the growth of the MOLM14 tumor in mice and, in Sprague-Dawley rats, shows favorable oral bioavailability and an acceptable half-life (T1/2 = 3.28 h). |
Molecular Weight | 494.03 |
Formula | C21H24ClN5O3S2 |
Cas No. | 2244992-76-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (91.09 mM) ![]() | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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