CAS No. 1035555-63-5
| IUPAC Name | 3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione | |
|---|---|---|
| CAS Number | 1035555-63-5 | |
| Molecular Formula |
C17H15F2IN4O4 |
|
| Molecular Weight (MW) | 504.23 | |
| SMILES | CN1C2=C(C(=C(C1=O)F)NC3=C(C=C(C=C3)I)F)C(=O)N(C=N2)CC(CO)O | |
| InChIKey | RCLQNICOARASSR-SECBINFHSA-N |
TAK-733 is a potent and selective allosteric inhibitor of MEK1 (IC50 3.2 nM). By blocking dual-specificity threonine/tyrosine kinase activity within the RAS/RAF/MEK/ERK pathway, TAK-733 suppresses cellular ERK phosphorylation (EC50 1.9 nM). This inhibition disrupts downstream effector proteins and transcription factors, leading to reduced growth factor-mediated signaling, impaired cell proliferation, and significant antitumor efficacy in mouse xenograft models. [1]
|
Concentration
Volume
Mass
|
|---|
| Solvent | Solubility & Note |
|---|---|
| DMSO |
101 mg/mL
(200.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
| DMSO |
101 mg/mL
(200.3 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO. The recommended stock concentration is 10 mM in DMSO.) |
| Water | Insoluble |
| Ethanol | Insoluble |
- Preheat media/saline to 37°C.
- Mix rapidly (pipette/vortex) upon addition.
- For complex mixes, always add the aqueous phase last.
- Re-dissolve minor precipitates with a 37°C water bath and sonication (≤30 min).
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