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Tinlorafenib

CAT: 0804-HY-147405-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-147405-01Size:1 mg
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
B-Raf

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CatalogName
T62841-01Tinlorafenib

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