生物活性
OSI-906是一种选择性IGF-1R抑制剂，在无细胞试验中IC50为35 nM；对InsR抑制作用适中，IC50为75 nM，对Abl，ALK，BTK，EGFR， FGFR1/2，PKA等没有抑制活性。
Targets
| Target | Value |
| IGF-1R | IC50: 35nM |
| Insulin Receptor | IC50: 75nM |
| IRR | IC50: 75nM |
| Abl | IC50: >10μM |
| ALK | IC50: >10μM |
| BTK | IC50: >10μM |
| EGFR | IC50: >10μM |
| EphA1 | IC50: >10μM |
| EphB1 | IC50: >10μM |
| FES | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| FGFR2 | IC50: >10μM |
| Fyn | IC50: >10μM |
| PKA | IC50: >10μM |
| PKCα | IC50: >10μM |
| ROCK1 | IC50: >10μM |
| IRAK4 | IC50: >10μM |
| JAK2 | IC50: >10μM |
| KDR | IC50: >10μM |
| LCK | IC50: >10μM |
| LynA | IC50: >10μM |
| LynB | IC50: >10μM |
| Met | IC50: >10μM |
| TrkA | IC50: >10μM |
| PDGFRα | IC50: >10μM |
| PDGFRβ | IC50: >10μM |
| FAK | IC50: >10μM |
| BRK | IC50: >10μM |
| RET | IC50: >10μM |
| Pim1 | IC50: >10μM |
| CDK1 | IC50: >10μM |
| DYRK2 | IC50: >10μM |
| Src | IC50: >10μM |
| Tek | IC50: >10μM |
| MEK1 | IC50: >10μM |
| Akt1 | IC50: >10μM |
| Akt2 | IC50: >10μM |
| AuroraA | IC50: >10μM |
| AuroraB | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| PLK1 | IC50: >10μM |
| p38α | IC50: >10μM |
| ERK1 | IC50: >10μM |
| GSK-3α | IC50: >10μM |
| p70S6K | IC50: >10μM |
化学数据
| 目录号 | A11053 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 421.5 |
| Formula | C26H23N5O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 867160-71-2 |
| Synonyms | OSI906, linsitinib |
| SMILES | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O |
溶解度
| In vitro (25°C) | DMSO | 80 mg/mL (189.8 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 5%DMSO+40%PEG300+5%Tween80+50%ddH2O | 5.93 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 23.72 mL | 118.62 mL | 237.25 mL |
| 0.5 mM | 4.74 mL | 23.72 mL | 47.45 mL |
| 1 mM | 2.37 mL | 11.86 mL | 23.72 mL |
| 5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
*The above data is based on the productmolecular weight 421.5 . 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.
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