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BEZ235 (NVP-BEZ235,Dactolisib)是通过与这些酶的ATP结合裂隙结合来抑制PI3K和mTOR激酶活性。
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.
| 目录号 | A10133 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 469.6 |
| Formula | C30H23N5O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 915019-65-7 |
| 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 |
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