生物活性
PHA-680632是Aurora A,Aurora B和Aurora C的有效抑制剂,IC50分别为27 nM,135 nM和120 nM。对于FGFR1,FLT3,LCK,PLK1,STLK2和VEGFR2/3,它的IC50高10到200倍。
Targets
Target |
Value |
AuroraA |
IC50: 27nM |
AuroraC |
IC50: 120nM |
AuroraB |
IC50: 135nM |
FGFR1 |
IC50: 390nM |
PLK1 |
IC50: 780nM |
FLT3 |
IC50: 820nM |
VEGFR3 |
IC50: 1000nM |
VEGFR2 |
IC50: 1920nM |
LCK |
IC50: 1950nM |
STLK2 |
IC50: 5500nM |
化学数据
目录号 |
A10714 |
作用机制 |
Inhibitor (抑制剂) |
M. Wt |
501.6 |
Formula |
C28H35N7O2 |
Purity |
>99% |
Storage |
Store lyophilized at -20?C, keep desiccated. In lyophilized form, the chemical is stable for36 months. In solution, store at -20?C and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
CAS No. |
398493-79-3 |
Synonyms |
PHA680632 |
SMILES |
CCC1=C(C(=CC=C1)CC)NC(=O)N2CC3=C(C2)NN=C3NC(=O)C4=CC=C(C=C4)N5CCN(CC5)C |
溶解度
In vitro (25°C) |
DMSO |
91 mg/mL (181.41 mM) |
Water |
Insoluble |
Ethanol |
Insoluble |
In vivo |
5% DMSO+50% PEG 300+5% Tween 80+ddH2O |
14 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 |
19.94 mL |
99.68 mL |
199.36 mL |
0.5 mM |
3.99 mL |
19.94 mL |
39.87 mL |
1 mM |
1.99 mL |
9.97 mL |
19.94 mL |
5 mM |
0.4 mL |
1.99 mL |
3.99 mL |
*The above data is based on the productmolecular weight 501.6 . 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.