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- Makoto Koyama, .et al. Low-dose trametinib and Bcl-xL antagonist have a specific antitumor effect in KRAS-mutated colorectal cancer cells, Int J Oncol, 2020, Sep 2 PMID: 32901840
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Dominik Schulz, .et al. HNSCC cells resistant to EGFR pathway inhibitors are hypermutated and sensitive to DNA damaging substances, Am J Cancer Res, 2016, 6(9): 1963-1975 PMID: 27725902
Biological Activity
BEZ235 (NVP-BEZ235) inhibits PI3K and mTOR kinase activity by binding to the ATP-binding cleft of these enzymes.
Targets
| Target | Value |
|---|---|
| p110α | IC50: 4nM |
| p110γ | IC50: 5nM |
| mTOR(p70S6K) | IC50: 6nM |
| p110δ | IC50: 7nM |
| ATR | IC50: 21nM |
| p110β | IC50: 75nM |
| EGFR/ErbB1 | IC50: >8.5μM |
| VEGFR1/FLT1 | IC50: >10μM |
| FLT3 | IC50: >10μM |
| IGF-1R | IC50: >10μM |
| EphB4 | IC50: >10μM |
| RET | IC50: >10μM |
| Tie-2 | IC50: >10μM |
| c-Met | IC50: >10μM |
| FGFR(K650E) | IC50: >10μM |
| FAK | IC50: >10μM |
| JAK2 | IC50: >10μM |
| c-Abl | IC50: >10μM |
| c-Src | IC50: >10μM |
| PKA | IC50: >10μM |
| Akt1/PKBα | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| B-Raf(V599E) | IC50: >10μM |
| CDK1 | IC50: >10μM |
| In vitro (25°C) | DMSO | <1 mg/mL | |
| Water | Insoluble | ||
| Ethanol | Warmed: 16 mg/mL (34.07 mM) | ||
| In vivo | NMP+PEG300 (10+90, v+v) | 28 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 | 21.29 mL | 106.47 mL | 212.95 mL |
| 0.5 mM | 4.26 mL | 21.29 mL | 42.59 mL |
| 1 mM | 2.13 mL | 10.65 mL | 21.29 mL |
| 5 mM | 0.43 mL | 2.13 mL | 4.26 mL |
*The above data is based on the productmolecular weight 469.6. 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 | A10133 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 915019-65-7 |
| Formula | C30H23N5O |
| M. Wt | 469.6 |
| Purity | >98% |
| SMILES | CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5 |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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