Biological Activity
Potent Raf kinase inhibitor (IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively). Also inhibits Abl-1, DDR2, EPHA2 and RET tyrosine kinase activity. Inhibits pERK formation and attenuates tumor growth in melanoma cell xenografts expressing the B-RafV600E mutation in vivo. Orally bioavailable.
Compound Libraries
ML 786 dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 611.48 |
| Formula | C29H29F3N4O3.2HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1237536-18-3 |
| PubChem ID | 90488999 |
| InChI Key | DNMWHXHMDZCGEX-GHVWMZMZSA-N |
| Smiles | O=C(N[C@@H]2CCC(C=CC(OC4=C(CC5)C(NC=C4)=NC5=O)=C3)=C3C2)C1=CC(C(F)(F)F)=CC(C(N)(C)C)=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 61.15 | 100 | |
| water | 61.15 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 611.48. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.64 mL | 8.18 mL | 16.35 mL |
| 5 mM | 0.33 mL | 1.64 mL | 3.27 mL |
| 10 mM | 0.16 mL | 0.82 mL | 1.64 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.33 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Gould et al (2011) Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J.Med.Chem. 54 1836 PMID: 21341678
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