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AP26113是一种有效的，选择性的ALK抑制剂，对野生型的功效为0.62 nM，对包括crizotinib耐药的L1196M系在内的多种突变体的活性也很强。在一组EML4-ALK或NPM-ALK阳性细胞系中，AP26113的IC50值为4-31 nM。
Targets
| Target | Value |
|---|---|
| ALK | IC50: 0.62nM |
| FER | IC50: 1.3nM |
| ROS/ROS1 | IC50: 1.9nM |
| FLT3 | IC50: 2.1nM |
| FES/FPS | IC50: 3.4nM |
| FAK/PTK2 | IC50: 3.8nM |
| BRK | IC50: 4.1nM |
| STK22D | IC50: 4.3nM |
| Chk2 | IC50: 6.5nM |
| RSK2 | IC50: 13nM |
| TYK/LTK | IC50: 13nM |
| YES | IC50: 19nM |
| PYK2 | IC50: 24nM |
| ErbB4 | IC50: 27nM |
| CLK1 | IC50: 29nM |
| CaMKIId | IC50: 29nM |
| Chk1 | IC50: 30nM |
| RSK1 | IC50: 30nM |
| RSK4 | IC50: 42nM |
| IRR/INSRR | IC50: 45nM |
| IGF-1R | IC50: 46nM |
| ARK5 | IC50: 47nM |
| CaMKIIg | IC50: 48nM |
| LRRK2 | IC50: 51nM |
| FRK | IC50: 52nM |
| FLT4 | IC50: 58nM |
| RET | IC50: 65nM |
| CaMKK2 | IC50: 83nM |
| MARK2 | IC50: 94nM |
| PKCnu | IC50: 95nM |
| PHKg2 | IC50: 108nM |
| LOK/STK10 | IC50: 123nM |
| BRSK2 | IC50: 125nM |
| MARK3 | IC50: 127nM |
| MARK1 | IC50: 127nM |
| FGFR1 | IC50: 128nM |
| EGFR | IC50: 129nM |
| BLK | IC50: 136nM |
| TSSK2 | IC50: 138nM |
| AuroraA | IC50: 146nM |
| JAK2 | IC50: 154nM |
| FGFR4 | IC50: 181nM |
| PKCmu/PKD1 | IC50: 197nM |
| Fyn | IC50: 198nM |
| Hck | IC50: 198nM |
| MLK1/MAP3K9 | IC50: 218nM |
| FGFR2 | IC50: 228nM |
| CLK2 | IC50: 240nM |
| Lyn | IC50: 241nM |
| PKD2/PRKD2 | IC50: 285nM |
| c-Src | IC50: 329nM |
| BRSK1 | IC50: 338nM |
| FGFR3 | IC50: 358nM |
| Fms | IC50: 358nM |
| Insulin Receptor | IC50: 395nM |
| SIK2/SNF1LK2/QIK | IC50: 466nM |
| FGR | IC50: 491nM |
| TAOK1 | IC50: 492nM |
| Abl1 | IC50: 500nM |
| LCK | IC50: 512nM |
| PLK1 | IC50: 611nM |
| BTK | IC50: 673nM[null] |
| In vitro (25°C) | DMSO | 40 mg/mL (75.61 mM) | |
| Water | Insoluble | ||
| Ethanol | 93 mg/mL (175.8 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 | 18.9 mL | 94.52 mL | 189.03 mL |
| 0.5 mM | 3.78 mL | 18.9 mL | 37.81 mL |
| 1 mM | 1.89 mL | 9.45 mL | 18.9 mL |
| 5 mM | 0.38 mL | 1.89 mL | 3.78 mL |
*The above data is based on the productmolecular weight 529.01. 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 | A11948 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 529.01 |
| Formula | C26H34ClN6O2P |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 1197958-12-5 |
| Synonyms | AP-26113 |
| SMILES | CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC |
1. Shiao et al., Anaplastic Lymphoma Kinase (ALK) Inhibitors: New Cancer Breakthroughs for Lung Cancer, J. Cancer. Res. Pract. 2011, 27(4), 143-156.
2. Rivera et al., Efficacy and pharmacodynamic analysis of AP26113, a potent and selective orally active inhibitor of Anaplastic Lymphoma Kinase (ALK). Cancer Res. 2010, 70(8), Suppl 1., AACR 101st Annual Meeting 2010.
3. Katayama et al., Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc. Natl. Acad. Sci. 2011, 108(18), 7535-7540. Pubmed ID: 21502504
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