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.
|Solubility (25°C)||DMSO ≥ 90 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 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
 Shruthi Kanthaje, et al. Hepatol Res. Sorafenib response in hepatocellular carcinoma: MicroRNAs as tuning forks
 Josep M Llovet, et al. J Hepatol. Novel advancements in the management of hepatocellular carcinoma in 2008
|Related Raf Products|
Exarafenib (KIN-2787) is a highly selective, potent, next-generation, pan-RAF inhibitor with activity across BRAF and RAS mutant human tumor cell models. Exarafenib has anticancer activity by suppression of downstream MAPK pathway signaling.
Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively.
Vemurafenib (PLX4032; RG7204; RO5185426) is a first-in-class selective B-RAF inhibitor that inhibits the activity of RAFV600E and c-RAF-1 with IC50 at 31 nM and 48 nM, respectively. Vemurafenib can induce autophagy.
LUT014, a B-Raf inhibitor with an IC50 value of 11.7 nM, was developed for the study of reducing acne-like lesions associated with EGFR inhibitors at restricted doses.
GNE-9815 is one of the most selective kinase inhibitors of RAF, targeting KRAS mutant cancers by combination of drugs.
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