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BI 2536是Plk1的选择性抑制剂，可在低纳摩尔浓度下抑制Plk1酶的活性。
Targets
| Target | Value |
|---|---|
| PLK1 | IC50: 0.83nM |
| PLK2 | IC50: 3.5nM |
| PLK3 | IC50: 9.0nM |
| PI3Kα | IC50: 2.407μM |
| Met | IC50: 4.754μM |
| Tie-2 | IC50: 6.549μM |
| HGFR | IC50: 9.5μM |
| ErbB4 | IC50: 9.908μM |
| Abl | IC50: >10μM |
| Axl | IC50: >10μM |
| AMPK | IC50: >10μM |
| AuroraA | IC50: >10μM |
| AuroraB | IC50: >10μM |
| βIRK | IC50: >10μM |
| B-Raf | IC50: >10μM |
| BTK | IC50: >10μM |
| CDK1/CyclinB1 | IC50: >10μM |
| CDK2/CyclinE | IC50: >10μM |
| Chk1 | IC50: >10μM |
| CK1 | IC50: >10μM |
| CK2 | IC50: >10μM |
| C-Raf | IC50: >10μM |
| CSK | IC50: >10μM |
| DYRK1A | IC50: >10μM |
| ECK | IC50: >10μM |
| ERK2 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| FGFR3 | IC50: >10μM |
| FLT1 | IC50: >10μM |
| FLT3 | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| Hek | IC50: >10μM |
| HER2 | IC50: >10μM |
| ITK | IC50: >10μM |
| JAK2 | IC50: >10μM |
| JAK3 | IC50: >10μM |
| JNK1 | IC50: >10μM |
| LCK | IC50: >10μM |
| Lyn | IC50: >10μM |
| MAPKAPK2 | IC50: >10μM |
| MEK1 | IC50: >10μM |
| MSK1 | IC50: >10μM |
| MKK1 | IC50: >10μM |
| NEK6 | IC50: >10μM |
| p38α | IC50: >10μM |
| p38β | IC50: >10μM |
| p38γ | IC50: >10μM |
| p38δ | IC50: >10μM |
| PAK2 | IC50: >10μM |
| PDGFRα | IC50: >10μM |
| PDGFRβ | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| PKA | IC50: >10μM |
| PKBα | IC50: >10μM |
| PKBβ | IC50: >10μM |
| PKCα | IC50: >10μM |
| PRAK | IC50: >10μM |
| RET | IC50: >10μM |
| ROCK2 | IC50: >10μM |
| RON | IC50: >10μM |
| S6K | IC50: >10μM |
| SGK | IC50: >10μM |
| Src | IC50: >10μM |
| Syk | IC50: >10μM |
| In vitro (25°C) | DMSO | 21 mg/mL (40.25 mM) | |
| Water | Insoluble | ||
| Ethanol | 98 mg/mL (187.86 mM) | ||
| In vivo | 30% PEG 400+0.5% Tween 80+5% Propylene glycol | 14 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 | 19.17 mL | 95.84 mL | 191.68 mL |
| 0.5 mM | 3.83 mL | 19.17 mL | 38.34 mL |
| 1 mM | 1.92 mL | 9.58 mL | 19.17 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.83 mL |
*The above data is based on the productmolecular weight 521.7. 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 | A10134 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 521.7 |
| Formula | C28H39N7O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 755038-02-9 |
| Synonyms | BI2536, BI-2536 |
| SMILES | CC[C@@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C |
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