生物活性
TSU-68 (Orantinib,SU6668)在无细胞试验中具有8 nM的Ki对PDGFR自磷酸化的最大效力,但也强烈抑制Flk-1和FGFR1反磷酸化,对IGF-1R,Met,Src, Lck,Zap70,Abl和CDK2; 不抑制EGFR。
靶点信息
PDGFRβ (Cell-free assay) | FGFR1 (Cell-free assay) | Flk1 (Cell-free assay) | | |
8 nM(Ki) | 1.2 μM(Ki) | 2.1 μM(Ki) | | |
化学数据
目录号 | A10953 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 310.4 |
Formula | C18H18N2O3 |
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. | 252916-29-3 |
Synonyms | TSU68 |
SMILES | CC1=C(NC(=C1CCC(=O)O)C)/C=C\2/C3=CC=CC=C3NC2=O |
溶解度
In vitro (25°C) | DMSO | 55 mg/mL (177.22 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 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 | 32.22 mL | 161.08 mL | 322.16 mL |
0.5 mM | 6.44 mL | 32.22 mL | 64.43 mL |
1 mM | 3.22 mL | 16.11 mL | 32.22 mL |
5 mM | 0.64 mL | 3.22 mL | 6.44 mL |
*The above data is based on the productmolecular weight 310.4 . 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.