生物活性
OSI-906是一种选择性IGF-1R抑制剂,在无细胞试验中IC50为35 nM;对InsR抑制作用适中,IC50为75 nM,对Abl,ALK,BTK,EGFR, FGFR1/2,PKA等没有抑制活性。
Targets
Target | Value |
IGF-1R | IC50: 35nM |
Insulin Receptor | IC50: 75nM |
IRR | IC50: 75nM |
Abl | IC50: >10μM |
ALK | IC50: >10μM |
BTK | IC50: >10μM |
EGFR | IC50: >10μM |
EphA1 | IC50: >10μM |
EphB1 | IC50: >10μM |
FES | IC50: >10μM |
FGFR1 | IC50: >10μM |
FGFR2 | IC50: >10μM |
Fyn | IC50: >10μM |
PKA | IC50: >10μM |
PKCα | IC50: >10μM |
ROCK1 | IC50: >10μM |
IRAK4 | IC50: >10μM |
JAK2 | IC50: >10μM |
KDR | IC50: >10μM |
LCK | IC50: >10μM |
LynA | IC50: >10μM |
LynB | IC50: >10μM |
Met | IC50: >10μM |
TrkA | IC50: >10μM |
PDGFRα | IC50: >10μM |
PDGFRβ | IC50: >10μM |
FAK | IC50: >10μM |
BRK | IC50: >10μM |
RET | IC50: >10μM |
Pim1 | IC50: >10μM |
CDK1 | IC50: >10μM |
DYRK2 | IC50: >10μM |
Src | IC50: >10μM |
Tek | IC50: >10μM |
MEK1 | IC50: >10μM |
Akt1 | IC50: >10μM |
Akt2 | IC50: >10μM |
AuroraA | IC50: >10μM |
AuroraB | IC50: >10μM |
PDK-1 | IC50: >10μM |
PLK1 | IC50: >10μM |
p38α | IC50: >10μM |
ERK1 | IC50: >10μM |
GSK-3α | IC50: >10μM |
p70S6K | IC50: >10μM |
化学数据
目录号 | A11053 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 421.5 |
Formula | C26H23N5O |
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. | 867160-71-2 |
Synonyms | OSI906, linsitinib |
SMILES | CC1(CC(C1)C2=NC(=C3N2C=CN=C3N)C4=CC5=C(C=C4)C=CC(=N5)C6=CC=CC=C6)O |
溶解度
In vitro (25°C) | DMSO | 80 mg/mL (189.8 mM) |
Water | Insoluble |
Ethanol | Insoluble |
In vivo | 5%DMSO+40%PEG300+5%Tween80+50%ddH2O | 5.93 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 | 23.72 mL | 118.62 mL | 237.25 mL |
0.5 mM | 4.74 mL | 23.72 mL | 47.45 mL |
1 mM | 2.37 mL | 11.86 mL | 23.72 mL |
5 mM | 0.47 mL | 2.37 mL | 4.74 mL |
*The above data is based on the productmolecular weight 421.5 . 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.