Braftide

Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAFG469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research[1][2].

Product Specifications

CAS Number

[2411851-64-2]

UNSPSC

12352209

Target

Raf

Type

Peptides

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/braftide.html

Purity

99.68

Solubility

DMSO : ≥ 100 mg/mL

Smiles

O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC1=CNC=N1)C(N[C@@H](C(C)C)C(N[C@@H](CC(N)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CC(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](CCSC)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H]([C@H](O)C)N

Molecular Formula

C57H94N16O13S

Molecular Weight

1243.52

References & Citations

[1]Gunderwala AY, et al., Development of Allosteric BRAF Peptide Inhibitors Targeting the Dimer Interface of BRAF. ACS Chem Biol. 2019 Jul 19;14 (7) :1471-1480. |[2]Yu A. Mechanistic Investigations of a Novel BRAF Regulatory Switch and Braftide, an Allosteric Peptide Inhibitor of BRAF[D]. Rowan University, 2023.