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MLN2480

Cat. No. M2090
MLN2480 Structure
Synonym:

BIIB-024; Tovorafenib

Size Price Availability Quantity
5mg USD 130  USD130 In stock
10mg USD 225  USD225 In stock
50mg USD 720  USD720 In stock
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Quality Control & Documentation
Biological Activity

MLN2480 (BIIB-024) is an oral, selective pan-Raf kinase inhibitor. MLN2480 inhibits signaling pathway at high concentrations in the human malignant melanoma A-375 mutant B-raf Val600Glu cell line. In vivo, MLN2480 showed antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models. At 20-200mg MLN2480 PK data (13 pts) exhibited rapid absorption (median Tmax 2 hr), low fluctuation at steady state (mean peak to trough ratio 2.1), and mean accumulation half-life of 67 hr. MLN2480 is currently in a phase I trial.

Chemical Information
Molecular Weight 506.29
Formula C17H12Cl2F3N7O2S
CAS Number 1096708-71-2
Solubility (25°C) DMSO 10 mM
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] Anthony Tabet, et al. Applying support-vector machine learning algorithms toward predicting host-guest interactions with cucurbit[7]uril

[2] Gautham Gampa, et al. Brain Distribution and Active Efflux of Three panRAF Inhibitors: Considerations in the Treatment of Melanoma Brain Metastases

[3] Yu Sun, et al. A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas

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Keywords: MLN2480, BIIB-024; Tovorafenib supplier, Raf, inhibitors, activators


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