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CHMFL-PI3KD-317

Catalog No. T10804Cas No. 2244992-76-3

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.

CHMFL-PI3KD-317

CHMFL-PI3KD-317

Purity: 97.8%
Catalog No. T10804Cas No. 2244992-76-3
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.
Pack SizePriceAvailabilityQuantity
1 mg$93In Stock
5 mg$228In Stock
10 mg$347In Stock
25 mg$625In Stock
50 mg$939In Stock
100 mg$1,280In Stock
1 mL x 10 mM (in DMSO)$248In Stock
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Purity:97.8%
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Product Introduction

Bioactivity
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
PI3Kδ:6 nM, VPS34:1801.7 nM, PI3Kβ:284 nM, PIK3C2B:882.3 nM, PI4KIIIA:574.1 nM, PI3Kα:62.6 nM, PI3Kγ:202.7 nM, PI4KIIIB:300.2 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).
Chemical Properties
Molecular Weight494.03
FormulaC21H24ClN5O3S2
Cas No.2244992-76-3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.0242 mL10.1208 mL20.2417 mL101.2084 mL
5 mM0.4048 mL2.0242 mL4.0483 mL20.2417 mL
10 mM0.2024 mL1.0121 mL2.0242 mL10.1208 mL
20 mM0.1012 mL0.5060 mL1.0121 mL5.0604 mL
50 mM0.0405 mL0.2024 mL0.4048 mL2.0242 mL

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