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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

Curated Selection

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