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Background Information:
CAL-101 is a PI3K/P110δ isoform-specific inhibitor with IC50 value of 2.5 nM, selective against other isoforms: p110α (820 nM), p110β (565 nM) and P110γ (89 nM).
Reference:
1. Lannutti BJ, Meadows SA, Herman SE, Kashishian A, Steiner B, Johnson AJ, Byrd JC, Tyner JW, Loriaux MM, Deininger M, Druker BJ, Puri KD, Ulrich RG, Giese NA. CAL-101, a p110{delta} selective phosphatidylinositol-3-kinase inhibitor (PI3K) for the treatment of B cell malignancies inhibits PI3K signaling and cellular viability. Blood. 2010 Oct 19. [Epub ahead of print].
2. Kahl BS, Cheson BD, Friedberg JW. Clinical Roundtable Monograph: current treatment options for NHL patients refractory to standard therapy: recent data in single-agent and combination therapy. Clin Adv Hematol Oncol. 2010 May;8(5):1-16.
3. Herman SE, Gordon AL, Wagner AJ, Heerema NA, Zhao W, Flynn JM, Jones J, Andritsos L, Puri KD, Lannutti BJ, Giese NA, Zhang X, Wei L, Byrd JC, Johnson AJ. Phosphatidylinositol 3-kinase-δ inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals. Blood. 2010 Sep 23;116(12):2078-88.
APIM050122: CAL-101
CAS No.: 870281-82-6.
Molecular Formula: C22H18FN7O? 0.3H2O.
Molecular Weight: 420.8.
Purity: >99% and >98.5% chem purity (HPLC at 254 nm and 214 nm); 99% optical purity (chiral HPLC).
QC: HPLC-MS, Chiral HPLC, 1HNMR and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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