Biological Activity
Mubritinib (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 µM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5.
Targets
Target | Value |
---|---|
HER2/ErbB2 | IC50: 6.0nM |
EGFR | IC50: >25μM |
FGFR | IC50: >25μM |
PDGFR | IC50: >25μM |
JAK1 | IC50: >25μM |
Src | IC50: >25μM |
BLK | IC50: >25μM |
In vitro (25°C) | DMSO | 12 mg/mL (25.61 mM) | |
Water | Insoluble | ||
Ethanol | Insoluble | ||
In vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80 | 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. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 21.34 mL | 106.72 mL | 213.45 mL |
0.5 mM | 4.27 mL | 21.34 mL | 42.69 mL |
1 mM | 2.13 mL | 10.67 mL | 21.34 mL |
5 mM | 0.43 mL | 2.13 mL | 4.27 mL |
*The above data is based on the productmolecular weight 468.5 . 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 | A10612 |
---|---|
Actions | Inhibitor |
CAS No. | 366017-09-6 |
Formula | C25H23F3N4O2 |
M. Wt | 468.5 |
Purity | >98% |
Synonyms | TAK-165, TAK165 |
SMILES | C1=CC(=CC=C1CCCCN2C=CN=N2)OCC3=COC(=N3)/C=C/C4=CC=C(C=C4)C(F)(F)F |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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