CAL-101

The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival. CAL-101 is a cell permeable inhibitor of the PI3K catalytic subunit p110delta (IC50 = 2.5 nM) that demonstrates 40- to 300-fold selectivity against other PI3K class I enzymes (IC50s = 820, 565, and 89 nM for p110alpha, beta, and gamma, respectively). At 1 µM it can block constitutive PI3K signaling in malignant B-cell lines and primary patient tumor cells, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase, and apoptosis. It has also been shown to inhibit the chemotaxis of chronic lymphocytic leukemia cells and to downregulate the secretion of chemokines triggered by B-cell receptor signaling.Formal Name: 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone. CAS Number: 870281-82-6. Synonyms: GS-1101, Idelalisib. Molecular Formula: C22H18FN7O. Formula Weight: 415.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 25 mg/ml, Ethanol: 15 mg/ml. lambdamax: 269, 311 nm. SMILES: FC1=CC=CC(N=C([C@@H](NC2=C(N=CN3)C3=NC=N2)CC)N4C5=CC=CC=C5)=C1C4=O. InChi Code: InChI=1S/C22H18FN7O/c1-2-15(28-20-18-19(25-11-24-18)26-12-27-20)21-29-16-10-6-9-14(23)17(16)22(31)30(21)13-7-4-3-5-8-13/h3-12,15H,2H2,1H3,(H2,24,25,26,27,28)/t15-/m0/s1. InChi Key: IFSDAJWBUCMOAH-HNNXBMFYSA-N.