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Tinlorafenib

Cat. No. M21640
Tinlorafenib Structure
Synonym:

PF-07284890; ARRY-461

Size Price Availability Quantity
5mg USD 640  USD640 In stock
10mg USD 1020  USD1020 In stock
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Quality Control & Documentation
Biological Activity

Tinlorafenib (PF-07284890) is an orally active BRAF kinase inhibitor, with IC50 values of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS.

Chemical Information
Molecular Weight 456.89
Formula C19H19ClF2N4O3S
CAS Number 2573781-75-4
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] Matthew Walton, et al. Health Technol Assess. Selective internal radiation therapies for unresectable early-, intermediate- or advanced-stage hepatocellular carcinoma: systematic review, network meta-analysis and economic evaluation

[2] Shruthi Kanthaje, et al. Hepatol Res. Sorafenib response in hepatocellular carcinoma: MicroRNAs as tuning forks

[3] Josep M Llovet, et al. J Hepatol. Novel advancements in the management of hepatocellular carcinoma in 2008

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Keywords: Tinlorafenib, PF-07284890; ARRY-461 supplier, Raf, inhibitors, activators


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