L-779450 suppressed DNA synthesis and induced apoptosis in hematopoietic FDC-P1 cells transformed to grow in response to either Raf-1 or A-Raf (FD/DeltaRaf-1:ER and FD/DeltaA-Raf:ER), but it displayed less effects on DNA synthesis and apoptosis when the cells were cultured in IL-3. L-779450 was less effective on B-Raf- or MEK1-responsive cells. Treatment with L779450, but not PLX4720, induced strong KSR1/B-Raf binding in A549 and HMCB cells that possess oncogenic Ras proteins, in the Cal12T line that contains an impaired activity B-Raf mutant, and, surprisingly, in A375 melanoma cells that are homozygous for V600E-B-Raf. L779450-induced B-Raf/C-Raf dimerization was not reduced in MEFs expressing the R615H- and C809Y-KSR1 mutants unable to bind B-Raf; whereas B-Raf/C-Raf dimerization was abolished in cells expressing S297A/S392A-KSR1 that exhibits enhanced inhibitor-induced B-Raf binding.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||≥ 34 mg/mL in DMSO|
The identification of potent, selective and CNS penetrant furan-based inhibitors of B-Raf kinase.
Takle AK, et al. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4373-6. PMID: 18621524.
Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation.
Shelton JG, et al. Leukemia. 2003 Sep;17(9):1765-82. PMID: 12970777.
|Related Raf Products|
PLX7904, also known as PB04, is a potent and selective paradox-breaker RAF inhibitor.
PLX8394 is an orally bioavailable, potent and selective Raf inhibitor with IC50 of 5 nM.
B-Raf-IN-1 (MDK36057) is a potent b-Raf inhibitor with IC50 of 24 nM.
RAF709 is a novel Raf kinase inhibitor with IC50 values of 0.4 and 1.5 nM for c-Raf and b-Raf, respectively.
Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
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