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GSK1838705A是一种小分子激酶抑制剂，其抑制IGF-IR和胰岛素受体的IC50分别为2.0和1.6 nmol/L。
Targets
| Target | Value |
|---|---|
| ALK | IC50: 0.5nM |
| Insulin Receptor | IC50: 1.6nM |
| IGF-1R | IC50: 2nM |
| RSK1 | IC50: 1.6μM |
| JNK3 | IC50: 2μM |
| B-Raf(V600E) | IC50: >2μM |
| JNK1 | IC50: 5μM |
| JAK3 | IC50: 5μM |
| JNK2 | IC50: 8μM |
| Akt1 | IC50: >10μM |
| Akt2 | IC50: >10μM |
| ALK5 | IC50: >10μM |
| AuroraA | IC50: >10μM |
| AuroraB | IC50: >10μM |
| CaMKK2 | IC50: >10μM |
| CDK2/CyclinA | IC50: >10μM |
| EGFR | IC50: >10μM |
| ErbB2 | IC50: >10μM |
| HGK | IC50: >10μM |
| IKK3 | IC50: >10μM |
| PAK1 | IC50: >10μM |
| PCTAIRE1 | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| PI3Kα | IC50: >10μM |
| PI3Kβ | IC50: >10μM |
| PI3Kδ | IC50: >10μM |
| PI3Kγ | IC50: >10μM |
| PKCε | IC50: >10μM |
| ROCK1 | IC50: >10μM |
| Src1 | IC50: >10μM |
| VEGFR2 | IC50: >10μM |
| YAK3 | IC50: >10μM |
| p70S6K | IC50: >10μM |
| JAK2 | IC50: 13μM |
| JAK1 | IC50: >25μM |
| ASK1 | IC50: >25μM |
| ErbB4 | IC50: >25μM |
| GSK-3β | IC50: >25μM |
| IKK1 | IC50: >25μM |
| IKK2 | IC50: >25μM |
| ITK | IC50: >25μM |
| LCK | IC50: >25μM |
| MAPKAPK2 | IC50: >25μM |
| p38α | IC50: >25μM |
| Syk | IC50: >25μM |
| ZAP70 | IC50: >25μM |
| In vitro (25°C) | DMSO | 103 mg/mL (193.4 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 15% Captisol+citrate vehicle | 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 | 18.78 mL | 93.88 mL | 187.77 mL |
| 0.5 mM | 3.76 mL | 18.78 mL | 37.55 mL |
| 1 mM | 1.88 mL | 9.39 mL | 18.78 mL |
| 5 mM | 0.38 mL | 1.88 mL | 3.76 mL |
*The above data is based on the productmolecular weight 532.57. 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 | A11175 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 532.57 |
| Formula | C27H29FN8O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 1116235-97-2 |
| Synonyms | GSK-1838705A |
| SMILES | CNC(=O)C1=C(C=CC=C1F)NC2=NC(=NC3=C2C=CN3)NC4=C(C=C5CCN(C5=C4)C(=O)CN(C)C)OC |
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