生物活性
BMS-754807是一种有效的,口服活性生长因子1受体/胰岛素受体家族靶向的激酶抑制剂。
Targets
Target | Value |
Insulin Receptor | IC50: 1.7nM |
IGF-1R | IC50: 1.8nM |
TrkB | IC50: 4.1nM |
Met | IC50: 5.6nM |
TrkA | IC50: 7.4nM |
AuroraA | IC50: 9nM |
AuroraB | IC50: 25nM |
RON | IC50: 44nM |
FLT3 | IC50: 170nM |
JAK2 | IC50: 347nM |
GSK-3β | IC50: 785nM |
CDK2E | IC50: 795nM |
MK2 | IC50: 919nM |
LCK | IC50: 1.218μM |
Src | IC50: 1.527μM |
PKA | IC50: 1.605μM |
PKCα | IC50: 2.53μM |
BTK | IC50: 3.797μM |
CSK | IC50: 5μM |
PKCδ | IC50: 12μM |
PKCζ | IC50: >50μM |
PKCι | IC50: >50μM |
p38α | IC50: >50μM |
p38β | IC50: >50μM |
HER1 | IC50: >50μM |
IKK1 | IC50: >50μM |
IKK2 | IC50: >50μM |
化学数据
目录号 | A11059 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 461.5 |
Formula | C23H24FN9O |
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. | 1001350-96-4 |
Synonyms | BMS754807, BMS 754807 |
SMILES | C[C@]1(CCCN1C2=NN3C=CC=C3C(=N2)NC4=NNC(=C4)C5CC5)C(=O)NC6=CN=C(C=C6)F |
溶解度
In vitro (25°C) | DMSO | 86 mg/mL (186.35 mM) |
Water | Insoluble |
Ethanol | 86 mg/mL |
In vivo | 2% DMSO+30% PEG 300+ddH2O | 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 | 21.67 mL | 108.34 mL | 216.68 mL |
0.5 mM | 4.33 mL | 21.67 mL | 43.34 mL |
1 mM | 2.17 mL | 10.83 mL | 21.67 mL |
5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
*The above data is based on the productmolecular weight 461.5 . 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.