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L-779450

Cat. No. M5327

L-779450 Structure
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 347.8
Formula C20H14ClN3O
CAS Number 303727-31-3
Purity >99%
Solubility ≥ 34 mg/mL in DMSO
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: L-779450 supplier, Raf, inhibitors

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