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| | CAL-101 Basic information |
| Product Name: | CAL-101 | | Synonyms: | CAL101,CAL-101;CAL-101;GS1101;CAL-101 (GS-1101);5-Fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone;CAL-101 (Idelalisib, GS-1101);(S)-2-(1-((9H-Purin-6-yl)aMino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one;4(3H)-Quinazolinone, 5-fluoro-3-phenyl-2-[(1S)-1-(1H-purin-6-ylaMino)propyl]- | | CAS: | 870281-82-6 | | MF: | C22H18FN7O | | MW: | 415.42 | | EINECS: | 807-438-9 | | Product Categories: | Akt;mTOR;PI3K;Inhibitors;Inhibitor;API;API | | Mol File: | 870281-82-6.mol |  |
| | CAL-101 Chemical Properties |
| Melting point | 250-252oC | | Boiling point | 733.4±70.0 °C(Predicted) | | density | 1.47 | | storage temp. | -20°C | | solubility | Soluble in DMSO (>25 mg/ml) | | form | White solid. | | pka | 10.00±0.10(Predicted) | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| | CAL-101 Usage And Synthesis |
| 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 | | 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. | | Definition | ChEBI: A member of the class of quinazolines that is 5-fluoro-3-phenylquinazolin-4-one in which the hydrogen at position 2 is replaced by a (1S)-1-(3H-purin-6-ylamino)propyl group. used for for the treatment of refractory indol
nt non-Hodgkin's lymphoma and relapsed chronic lymphocytic leukemia. | | target | p110δ | | storage | Store at -20°C | | References | 1) Herman?et al. (2010), Phosphatidylinositol 2-kinase-d inhibitor CAL-101 shows promising preclinical activity in chronic lymphocytic leukemia by antagonizing intrinsic and extrinsic cellular survival signals; Blood?116 2078
2) Lannutti?et al. (2011), CAL-101, a p110d selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability; Blood 117 591
3) Ahmad?et al. (2017), Differential PI3Kd Signaling in CD4+ T-cell Subsets Enables Selective Targeting of T Regulatory Cells to Enhance Cancer Immunotherapy; Cancer Res. 77 1892
4) Lim?et al. (2018), Phosphoinositide 3-kinase d inhibition promotes antitumor responses but antagonizes checkpoint inhibitors; JCI Insight 3 e120626
5) Palazzo?et al.?(2018),?The PI3Kd-Selective Inhibitor Idelalisib Minimally Interferes with Immune Effector Function Mediated by Rituximab or Obinutuzumab and Significantly Augment B Cell Depletion In Vivo; J.Immunol. 200 2304 |
| | CAL-101 Preparation Products And Raw materials |
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