- Li Li, .et al. Evidence for activated Lck protein tyrosine kinase as the driver of proliferation in acute myeloid leukemia cell, CTV-1, Leukemia Res, 2019, 78:12-20 PMID: 30660961
Biological Activity
BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.
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 |
In vitro (25°C) | DMSO | 92 mg/mL (199.35 mM) | |
Water | <1 mg/mL (<1 mM) | ||
Ethanol | 92 mg/mL (199.35 mM) | ||
In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 20 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. |
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.
Catalog Num | A11059 |
---|---|
Actions | Inhibitor |
M. Wt | 461.5 |
Formula | C23H24FN9O |
Solubility | DMSO |
Purity | >98% |
Storage | at -20°C 3 years Powder |
CAS No. | 1001350-96-4 |
Synonyms | BMS754807, BMS 754807 |
SMILES | C[[email protected]]1(CCCN1C2=NN3C=CC=C3C(=N2)NC4=NNC(=C4)C5CC5)C(=O)NC6=CN=C(C=C6)F |
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