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TAK-285是一种研究性的HER2/EGFR抑制剂，可在具有完整血脑屏障 (BBB) 的大鼠中穿透CNS。TAK-285对HER2和EGFR激酶具有抑制活性，HER2和EGFR的IC50值分别为17 nmol/L (95％CI 12-24)和23 nmol/L (95％CI 18-30)。
Targets
| Target | Value |
|---|---|
| HER2 | IC50: 17nM |
| EGFR/HER1 | IC50: 23nM |
| HER4 | IC50: 260nM |
| MEK1 | IC50: 1.1μM |
| AuroraB | IC50: 1.7μM |
| LCK | IC50: 2.4μM |
| c-Met | IC50: 4.2μM |
| CSK | IC50: 4.7μM |
| LynB | IC50: 5.2μM |
| MEK5 | IC50: 5.7μM |
| LynA | IC50: >10μM |
| FAK | IC50: >10μM |
| VEGFR1 | IC50: >10μM |
| VEGFR2 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| FGFR3 | IC50: >10μM |
| PDGFRα | IC50: >10μM |
| PDGFRβ | IC50: >10μM |
| IRK | IC50: >10μM |
| Tie-2 | IC50: >10μM |
| c-Kit | IC50: >10μM |
| IGF-1R | IC50: >10μM |
| Src | IC50: >10μM |
| ASK1 | IC50: >10μM |
| TAK1 | IC50: >10μM |
| MEKK1 | IC50: >10μM |
| IKKβ | IC50: >10μM |
| JNK1 | IC50: >10μM |
| ERK1 | IC50: >10μM |
| p38α | IC50: >10μM |
| PKA | IC50: >10μM |
| PKCθ | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| B-Raf | IC50: >10μM |
| TTK | IC50: >10μM |
| PLK1 | IC50: >10μM |
| In vitro | DMSO | 97 mg/mL (177.02 mM) | |
| Water | Insoluble | ||
| Ethanol | 48 mg/mL (87.59 mM) | ||
|
* <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 | 18.25 mL | 91.24 mL | 182.48 mL |
| 0.5 mM | 3.65 mL | 18.25 mL | 36.5 mL |
| 1 mM | 1.82 mL | 9.12 mL | 18.25 mL |
| 5 mM | 0.36 mL | 1.82 mL | 3.65 mL |
*The above data is based on the productmolecular weight 548.0 . 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 | A11236 |
|---|---|
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 548.0 |
| Formula | C26H25ClF3N5O3 |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
| CAS No. | 871026-44-7 |
| Synonyms | TAK285 |
| SMILES | CC(C)(CC(=O)NCCN1C=CC2=C1C(=NC=N2)NC3=CC(=C(C=C3)OC4=CC=CC(=C4)C(F)(F)F)Cl)O |
1. Shinji Takagi, Hiroshi Banno, Akira Hayashi, Toshiya Tamura, Tomoyasu Ishikawa, Yoshikazu Ohta., HER2 and HER3 cooperatively regulate cancer cell growth and determine sensitivity to the novel investigational EGFR/HER2 kinase inhibitor TAK-285. Oncoscience, 2014. 1(3): p. 196-204.
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