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> Pathway Inhibitors>Enzyme Inhibitors>Kinase Inhibitors>CHMFL-PI3KD-317

Kinase Inhibitors

CHMFL-PI3KD-317 View larger

CHMFL-PI3KD-317

AT10804

CAS 2244992-76-3

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$79.00

$79.00 per mg

Quantity Discount Table - Order More To Get More Price Discount

QuantitymgUnit Price ($/mg or $/Unit)Final Price
15 $67.15 Total: $335.75
110 $56.88 Total: $568.80
125 $48.19 Total: $1,204.75
150 $41.08 Total: $2,054.00
1100 $35.55 Total: $3,555.00

Data sheet

Molecular FormulaC21H24ClN5O3S2
Molecular Weight494.03
CAS Numbers2244992-76-3
Storage Condition0C Short Term, -20C Long Term
SolubilityDMSO
Purity98% by HPLC
SMILES CodeCC(C)[C@H](N)C(=O)Nc1nc(C)c(s1)-c1cnc(Cl)c(NS(=O)(=O)c2cccc(C)c2)c1
ReferencesLiang X, et al. Discovery of [S]-2-amino-N-[5-[6-chloro-5-[3-methylphenylsulfonamido]pyridin-3-yl]-4-methylthiazol-2-yl]-3-methylbutanamide [CHMFL-PI3KD-317] as a potent and selective phosphoinositide 3-kinase delta [PI3K?] inhibitor. Eur J Med Chem. 2018 Aug 5;156 831-846.

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CHMFL-PI3KD-317 is a highly potent, selective, and orally active PI3K? 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 PI3K? (IC50, 62.6 nM), PI3K? (IC50, 284 nM), PI3K? (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 PI3K?-mediated Akt T308 phosphorylation in Raji cells with an EC50 of 4.3 nM and has antiproliferative effects on cancer cells.