2573781-75-4
Chemical Structure
Tinlorafenib
Synonym(s): PF-07284890; ARRY-461
- CAS No.: 2573781-75-4
- Formula:C19H19ClF2N4O3S
- Molecular Weight:456.89
IUPAC Name: N-(2-chloro-3-((3,5-dimethyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino)-4-fluorophenyl)-3-fluoropropane-1-sulfonamide
InChIKey: VVLVISDSGRHLMB-UHFFFAOYSA-N
SMILES: O=C1C2=C(C=CC(NC3=C(Cl)C(NS(=O)(CCCF)=O)=CC=C3F)=C2C)N=CN1C
Biological Activity: 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].
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Tinlorafenib | 98.21% | 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. | ||||||||||||||||||||
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- [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.
Keywords
