Tinlorafenib

Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC50s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC50s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies[1][2].

Product Specifications

CAS Number

[2573781-75-4]

Product Name Alternative

PF-07284890; ARRY-461

UNSPSC

12352005

Target

ERK; Raf

Type

Reference compound

Related Pathways

MAPK/ERK Pathway; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tinlorafenib.html

Concentration

10mM

Purity

98.21

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

O=C1C2=C(C=CC(NC3=C(Cl)C(NS(=O)(CCCF)=O)=CC=C3F)=C2C)N=CN1C

Molecular Formula

C19H19ClF2N4O3S

Molecular Weight

456.89

References & Citations

[1]Barbour, et al. Quinazolin-4-one derivatives useful for the treatment of braf-associated diseases and disorders. WO2020261156A1. |[2]Bouhana K, et al. Nonclinical development of PF-07284890 (ARRY-461), a potent, brain-penetrant, small molecule inhibitor of BRAF V600-mutation-driven tumors in vitro and in vivo[J]. Cancer Research, 2021, 81 (13_Supplement) : 1473-1473.