PROTAC BRAF-V600E degrader-2
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth[1].
Product Specifications
CAS Number
[2417296-82-1]
UNSPSC
12352005
Target
PROTACs; Raf
Type
Reference compound
Related Pathways
MAPK/ERK Pathway; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/protac-braf-v600e-degrader-2.html
Solubility
10 mM in DMSO
Smiles
O=C(NCC1=CC=C(C2=CN=C(NC=C3C(C4=C(F)C=CC(NS(=O)(CCC)=O)=C4F)=O)C3=C2)C=C1)CCCCNC5=CC6=C(C(N(C(CC7)C(NC7=O)=O)C6=O)=O)C=C5
Molecular Formula
C42H39F2N7O8S
Molecular Weight
839.86
References & Citations
[1]Xiao-Ran Han, et al. Discovery of Selective Small Molecule Degraders of BRAF-V600E. J Med Chem. 2020 Apr 23;63 (8) :4069-4080.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
B-Raf; Cereblon
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