生物活性
AEE788是一种口服生物可用的多受体酪氨酸激酶抑制剂,可抑制EGFR,HER2和VEGF2酪氨酸激酶的磷酸化。
Targets
Target | Value |
EGFR | IC50: 2nM |
HER2/ErbB2 | IC50: 6nM |
c-Abl | IC50: 52nM |
FLT1 | IC50: 59nM |
c-Fms | IC50: 60nM |
c-Src | IC50: 61nM |
KDR | IC50: 77nM |
HER4/ErbB4 | IC50: 160nM |
PDGFRβ | IC50: 320nM |
FLT4 | IC50: 330nM |
FLT3 | IC50: 730nM |
RET | IC50: 740nM |
c-Kit | IC50: 790nM |
Tek | IC50: 2.1μM |
C-Raf-1 | IC50: 2.8μM |
c-Met | IC50: 2.9μM |
CDK1/CyclinB | IC50: 8.0μM |
IGF-1R | IC50: >10μM |
Insulin Receptor | IC50: >10μM |
PKCα | IC50: >10μM |
PKA | IC50: >10μM |
化学数据
目录号 | A10043 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 440.6 |
Formula | C27H32N6 |
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. | 497839-62-0 |
Synonyms | AEE-788, NVP-AEE788 |
SMILES | CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4N[C@H](C)C5=CC=CC=C5 |
溶解度
In vitro (25°C) | DMSO | 81 mg/mL (183.84 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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. |
储备液配制
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
0.1 mM | 22.7 mL | 113.48 mL | 226.96 mL |
0.5 mM | 4.54 mL | 22.7 mL | 45.39 mL |
1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
*The above data is based on the productmolecular weight 440.6 . 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.