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- Hiroshi Fukamachi, .et al. A subset of diffuse-type gastric cancer is susceptible to mTOR inhibitors and checkpoint inhibitors, J Exp Clin Cancer Res, 2019, 38:127
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
Biological Activity
PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
Targets
| Target | Value |
|---|---|
| mTOR | IC50: 8nM |
| p110δ | IC50: 0.10μM |
| DNA-PK | IC50: 0.41μM |
| PDGFR | IC50: 0.41μM |
| Hck | IC50: 1.2μM |
| p110γ | IC50: 1.3μM |
| Src | IC50: 1.4μM |
| VEGFR2 | IC50: 1.5μM |
| p110α | IC50: 2.0μM |
| p110β | IC50: 2.2μM |
| EphB4 | IC50: 3.4μM |
| Abl | IC50: 3.6μM |
| EGFR | IC50: 4.4μM |
| Src(T338I) | IC50: 5.1μM |
| In vitro (25°C) | DMSO | 57 mg/mL (184.86 mM) | |
| Water | Insoluble | ||
| Ethanol | 17 mg/mL (55.13 mM) | ||
| In vivo | 2% DMSO+30% PEG 300+5% Tween 80+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 | 32.44 mL | 162.18 mL | 324.36 mL |
| 0.5 mM | 6.49 mL | 32.44 mL | 64.87 mL |
| 1 mM | 3.24 mL | 16.22 mL | 32.44 mL |
| 5 mM | 0.65 mL | 3.24 mL | 6.49 mL |
*The above data is based on the productmolecular weight 308.3 . 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 | A10746 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 1092351-67-1 |
| Formula | C16H16N6O |
| M. Wt | 308.3 |
| Purity | >98% |
| Synonyms | PP-242 |
| SMILES | CC(C)N1C2=C(/C(=C\3/C=C4C=C(C=CC4=N3)O)/N1)C(=NC=N2)N |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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