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Belvarafenib

  Cat. No.:  DC12278   Featured
Chemical Structure
1446113-23-0
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More than 5000 active chemicals with high quality for research!
Field of application
Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1446113-23-0
Chemical Name: 4-Amino-N-(1-(3-chloro-2-fluorophenylamino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide
SMILES: O=C(C(C1=NC=N2)=CSC1=C2N)NC(C3=C4C(NC(C=CC=C5Cl)=C5F)=NC=C3)=C(C=C4)C
Formula: C23H16ClFN6Os
M.Wt: 478.93
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: TW Kim et al. Belvarafenib, a novel pan-RAF inhibitor, in solid tumor patients harboring BRAF, KRAS, or NRAS mutations: Phase I study. Journal of Clinical Oncology 37, no. 15_suppl (May 20, 2019) 3000-3000.
Description: Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.
In Vitro: Belvarafenib (Example 116) is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. It also shows high inhibitory activity for FMS, DDR1 and DDR2 kinases, with IC50s of 10 nM, 23 nM and 44 nM, respectively[1].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC71910 Tinlorafenib Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s 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 as well as extracranial malignancies[1].
DC71909 Exarafenib Exarafenib (RAF/KIN_2787) is a potent, orally active pan-RAF inhibitor. Exarafenib has anticancer activity by suppression of downstream MAPK pathway signaling. Exarafenib can be used for cancer research.
DC70702 PLX8394 PLX8394 (PLX-8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF (V600E), WT BRAF and CRAF, respectively.PLX8394 suppresses mutant BRAF cells without activating the MAPK pathway in cells bearing upstream activation, overcame several known mechanisms of resistance to first-generation RAF inhibitors.PLX8394 inhibits ERK signaling by specifically disrupting BRAF-containing dimers, including BRAF homodimers and BRAF-CRAF heterodimers, but not CRAF homodimers or ARAF-containing dimers.As a BRAF-specific dimer breaker, PLX8394 selectively inhibits ERK signaling in tumors driven by dimeric BRAF mutants, including BRAF fusions and splice variants as well as BRAF V600 monomers, but spares RAF function in normal cells in which CRAF homodimers can drive signaling.
DC39085 Donafenib (Sorafenib D3) Sorafenib D3 (Bay 43-9006 D3) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively.
DC7370 AZ-628 Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM For c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity For Raf kinases over a panel of 150 other kinases.
DC8727 PF-04880594 PF-04880594 is an inhibitor of RAF with IC50 values of 0.19 nM/0.13 nM and 0.39 nM for BRAF/BRAFV599E and c-RAF, respectively.
DC12278 Belvarafenib Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.
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