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B-Raf IN 13

Cat. No. M42153
B-Raf IN 13 Structure
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Biological Activity

B-Raf IN 13 is a BRAF inhibitor with an IC50 of 3.55 nM in BRAF V600E enzyme assay.

Chemical Information
Molecular Weight 439.89
Formula C19H19ClFN3O4S
CAS Number 2573782-74-6
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Ming Ren et al. Bioengineered. Overcoming chemoresistance to b-raf inhibitor in melanoma via targeted inhibition of phosphoenolpyruvate carboxykinase1 using 3-mercaptopropionic acid

[2] Francesco Calvanese et al. Front Endocrinol (Lausanne). Neoadjuvant B-RAF and MEK Inhibitor Targeted Therapy for Adult Papillary Craniopharyngiomas: A New Treatment Paradigm

[3] Claudia Capparelli et al. Nat Commun. Targeting SOX10-deficient cells to reduce the dormant-invasive phenotype state in melanoma

[4] Stefania Acciardo et al. J Cell Mol Med. Metabolic imaging using hyperpolarized 13 C-pyruvate to assess sensitivity to the B-Raf inhibitor vemurafenib in melanoma cells and xenografts

[5] James Tsai et al. Proc Natl Acad Sci U S A. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

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  Catalog
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