SB590885
SB590885 is a potent and selective inhibitor of B-Raf kinase with Ki value of 0.16nM [1].
SB590885 is a potent inhibitor of oncogenic B-Raf protein kinase with Ki value of 0.16nM. It is more potent to inhibit B-Raf than C-Raf. The Ki value of SB590885 for C-Raf is 1.72nM. SB590885 is a quite selective inhibitor. It shows no activity against 48 other human kinases such as Abl, AMPK, CK1, CK2 and ERK2. It is found that SB590885 binds to B-Raf within the ATP-binding pocket and stabilizes the active conformation of B-Raf. SB590885 decreases the phosphorylation of ERK and shows anti-proliferation only in tumor cells expressing oncogenic B-Raf V600E. The normal cells and tumor cells not expressing mutant B-Raf have no sensitivity towards SB590885 except the normal melanocytes and primary melanoma cells expressing wild-type B-Raf. Moreover, SB590885 is also found to decrease the transformed and tumorigenic properties of malignant cells expressing mutant B-Raf [1].
References:
[1] King A J, Patrick D R, Batorsky R S, et al. Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. Cancer research, 2006, 66(23): 11100-11105.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 453.55 |
| Cas No. | 405554-55-4 |
| Formula | C27H27N5O2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥4.54 mg/mL in DMSO with gentle warming |
| Chemical Name | N,N-dimethyl-2-[4-[(4Z)-4-(1-nitroso-2,3-dihydroinden-5-ylidene)-5-(1H-pyridin-4-ylidene)-1H-imidazol-2-yl]phenoxy]ethanamine |
| SDF | Download SDF |
| Canonical SMILES | CN(C)CCOC1=CC=C(C=C1)C2=NC(=C3C=CC4=C(CCC4=C3)N=O)C(=C5C=CNC=C5)N2 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | SB590885 is a potent inhibitor of B-Raf with a Ki value of 0.16 nM. | |||||
| Targets | B-Raf | |||||
| IC50 | 0.16 nM | |||||
Quality Control & MSDS
- View current batch:
Chemical structure
