生物活性
Neratinib (HKI-272)是一种酪氨酸激酶抑制剂。
Targets
Target | Value |
HER2 | IC50: 59nM |
EGFR | IC50: 92nM |
KDR | IC50: 800nM |
Src | IC50: 1.4μM |
PDK-1 | IC50: >5μM |
IKK2 | IC50: >9μM |
CDK2/CyclinE | IC50: >18μM |
CDK1/CyclinB1 | IC50: >18μM |
C-Raf/MEK1 | IC50: >18μM |
Tpl-2 | IC50: >18μM |
Akt | IC50: >20μM |
c-Met | IC50: >35μM |
MK2 | IC50: >45μM |
CDK4/CyclinD1 | IC50: >50μM |
化学数据
目录号 | A10638 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 557.0 |
Formula | C30H29ClN6O3 |
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. | 698387-09-6 |
SMILES | CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C |
溶解度
In vitro (25°C) | DMSO | Warmed: 4 mg/mL (7.18 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 4 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 | 17.95 mL | 89.77 mL | 179.53 mL |
0.5 mM | 3.59 mL | 17.95 mL | 35.91 mL |
1 mM | 1.8 mL | 8.98 mL | 17.95 mL |
5 mM | 0.36 mL | 1.8 mL | 3.59 mL |
*The above data is based on the productmolecular weight 557.0 . 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.