Chemical Property of Idelalisib
Chemical Property:
- Melting Point:250-252oC
- Boiling Point:733.4±70.0 °C(Predicted)
- PKA:10.00±0.10(Predicted)
- PSA：101.38000
- Density:1.47
- LogP:3.82730
- Storage Temp.:-20°C
- Solubility.:Soluble in DMSO (>25 mg/ml)
- XLogP3:3.7
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:5
- Exact Mass:415.15568639
- Heavy Atom Count:31
- Complexity:685
- Purity/Quality:
-
99% *data from raw suppliers
CAL-101 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- Safety Statements:
V
- MSDS Files:
-
SDS file from LookChem
Useful:
- Drug Classes:Antineoplastic Agents
- Canonical SMILES:CCC(C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
- Isomeric SMILES:CC[C@@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5
- Recent ClinicalTrials:Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) PRIME Trial
- Recent EU Clinical Trials:A Phase 2 Randomized Study of Loncastuximab Tesirine Versus Idelalisib in Patients with Relapsed or Refractory Follicular Lymphoma (LOTIS 6)
- Recent NIPH Clinical Trials:A Phase 3 Study of LOXO-305 in Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma
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Description
Idelalisib (CAS 870281-82-6) is a potent (IC50 = 2.5nM) and selective (IC50’s: PI3Ka = 820nM, PI3Kb = 565nM, PI3Kg = 89nM) PI3Kd inhibitor.1,2 Useful clinical agent for the treatment of various blood cancers. Idelalisib attenuates regulatory T cells (Treg) but not conventional T cells (Tconv) resulting in a significant increase in tumor-infiltrating antigen-specific CD8 T cells in a murine lung cancer model.3 Conversely, systemic PI3Kd inactivation antagonized anti-CTLA-4 and anti-PD-L1 treatment.4 Others have found that Idelalisib minimally influenced rituximab- and obinutuzumab-mediated Ab-dependent cellular cytotoxicity in human lymphoma cells.5
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Uses
CAL-101 is a PI3K/mTOR pathway inhibitor used in the treatment of myeloid leukemia through sensitizing the cells to combatting drugs. Potent PI3K-p110-delta inhibitor.
