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- Ming-Chun Hung, .et al. AKT phosphorylation as a predictive biomarker for PI3K/mTOR dual inhibition-induced proteolytic cleavage of mTOR companion proteins in small cell lung cancer, Cell Biosci, 2022, 12: 122 PMID: 35918763
- Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Pridham KJ, .et al. PIK3CB/p110β is a selective survival factor for glioblastoma, Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
- Yoshihiro Umezawa, .et al. Molecular mechanisms for enhancement of stromal cell-derived factor 1?Cinduced chemotaxis by platelet endothelial cell adhesion molecule 1 (PECAM-1), J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577
Biological Activity
CAL-101 is an isoform-selective inhibitor of PI3K that induces apoptosis of chronic lymphocytic leukemia (CLL) cells.
Targets
| Target | Value |
|---|---|
| p110δ | IC50: 2.5nM |
| p110γ | IC50: 89nM |
| p110β | IC50: 565nM |
| p110α | IC50: 820nM |
| hVps34 | IC50: 978nM |
| C2β | IC50: >1μM |
| mTOR | IC50: >1μM |
| PIP5Kα | IC50: >1μM |
| PIP5Kβ | IC50: >1μM |
| DNA-PK | IC50: 6.729μM |
| In vitro (25°C) | DMSO | Warmed: 76 mg/mL (182.94 mM) | |
| Water | Insoluble | ||
| Ethanol | 21 mg/mL (50.55 mM) | ||
| In vivo | 2% DMSO+20%PEG 300+ddH2O | 4 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 24.07 mL | 120.37 mL | 240.73 mL |
| 0.5 mM | 4.81 mL | 24.07 mL | 48.15 mL |
| 1 mM | 2.41 mL | 12.04 mL | 24.07 mL |
| 5 mM | 0.48 mL | 2.41 mL | 4.81 mL |
*The above data is based on the productmolecular weight 415.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10172 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 870281-82-6 |
| Formula | C22H18FN7O |
| M. Wt | 415.4 |
| Purity | >98% |
| Synonyms | CAL101 |
| SMILES | CC[[email protected]@H](C1=NC2=C(C(=CC=C2)F)C(=O)N1C3=CC=CC=C3)NC4=NC=NC5=C4NC=N5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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