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Literature summary for 2.7.1.153 extracted from

  • Lannutti, B.J.; Meadows, S.A.; Herman, S.E.; Kashishian, A.; Steiner, B.; Johnson, A.J.; Byrd, J.C.; Tyner, J.W.; Loriaux, M.M.; Deininger, M.; Druker, B.J.; Puri, K.D.; Ulrich, R.G.; Giese, N.A.
    CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability (2011), Blood, 117, 591-594.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.153

Inhibitors

Inhibitors Comment Organism Structure
3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one i.e. CAL-101, highly selective and small molecule inhibitor of isoform PI3Kdelta. Inhibitor blocks constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens O00329 catalytic subunit delta isoform
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000025
-
 isoform PI3Kdelta, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one
0.000089
-
 isoform PI3Kgamma, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one
0.000565
-
 isoform PI3Kbeta, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one
0.00082
-
 isoform PI3Kalpha, pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one

General Information

General Information Comment Organism
physiological function in tumor cell lines and primary patient samples representing multiple B-cell malignancies, constitutive phosphatidylinositol-3-kinase pathway activation is dependent on isoform PI3Kdelta. Inhibitor 3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one blocks constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis Homo sapiens