生物活性
Linifanib (ABT-869)是一种结构新颖的有效RTK,VEGF和PDGF抑制剂,对人内皮细胞,PDGFR-β,KDR和CSF-1R的IC50分别为0.2、2、4和7 nM。
Targets
Target | Value |
VEGFR1/FLT1 | IC50: 3nM |
CSF-1R | IC50: 3nM |
VEGFR2/KDR | IC50: 4nM |
FLT3 | IC50: 4nM |
Kit | IC50: 14nM |
PDGFRβ | IC50: 66nM |
Tie-2 | IC50: 170nM |
VEGFR3/FLT4 | IC50: 190nM |
SGK | IC50: 940nM |
RET | IC50: 1.9μM |
PKA | IC50: 5.9μM |
Cdc2 | IC50: 9.8μM |
FGFR | IC50: >12.5μM |
Lyn | IC50: >20μM |
LCK | IC50: 38μM |
Src | IC50: >50μM |
IGFR | IC50: >50μM |
INSR | IC50: >50μM |
EGFR | IC50: >50μM |
Hck | IC50: >50μM |
c-Met | IC50: >50μM |
Fyn | IC50: >50μM |
FGR | IC50: >50μM |
Akt | IC50: >50μM |
化学数据
目录号 | A10025 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 375.4 |
Formula | C21H18FN5O |
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. | 796967-16-3 |
Synonyms | ABT869, ABT-869 |
SMILES | CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N |
溶解度
In vitro (25°C) | DMSO | 73 mg/mL (194.45 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 5%DMSO+40%PEG 300+5%Tween80+50%ddH2O | 9 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 | 26.64 mL | 133.19 mL | 266.38 mL |
0.5 mM | 5.33 mL | 26.64 mL | 53.28 mL |
1 mM | 2.66 mL | 13.32 mL | 26.64 mL |
5 mM | 0.53 mL | 2.66 mL | 5.33 mL |
*The above data is based on the productmolecular weight 375.4 . 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.