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LGX818

Cat. No. M2813
LGX818 Structure
Synonym:

Encorafenib

Size Price Availability Quantity
2mg USD 65  USD65 In stock
5mg USD 90  USD90 In stock
10mg USD 150  USD150 In stock
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Quality Control & Documentation
Biological Activity

LGX818 is a highly potent RAF inhibitor with selective anti-proliferative and apoptotic activity in cells expressing B-RAF(V600E) with EC50 of 4 nM.

Chemical Information
Molecular Weight 540.01
Formula C22H27ClFN7O4S
CAS Number 1269440-17-6
Solubility (25°C) DMSO 90 mg/mL
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] Josep Tabernero, et al. Encorafenib Plus Cetuximab as a New Standard of Care for Previously Treated BRAF V600E-Mutant Metastatic Colorectal Cancer: Updated Survival Results and Subgroup Analyses from the BEACON Study

[2] Rahul Seth, et al. Systemic Therapy for Melanoma: ASCO Guideline

[3] Scott Kopetz, et al. Encorafenib, Binimetinib, and Cetuximab in BRAF V600E-Mutated Colorectal Cancer

[4] Lucie Heinzerling, et al. Tolerability of BRAF/MEK inhibitor combinations: adverse event evaluation and management

[5] Paola Savoia, et al. Targeting the ERK Signaling Pathway in Melanoma

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  Catalog
Abmole Inhibitor Catalog




Keywords: LGX818, Encorafenib supplier, Raf, inhibitors, activators


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