VVD-699

VVD-699 is a covalent RAS-PI3K inhibitor. VVD-699 covalently binds to cysteine 242 in the RAS binding domain of PI3K p110α, thereby blocking the ability of RAS to activate PI3K activity. VVD-699 is able to inhibit the growth of RAS-mutated and HER2-overexpressing tumors. VVD-699 can be used to study cancers associated with RAS mutations (e.g., H358 lung cancer cells, A549 cells, FaDu cells) [1].

Product Specifications

CAS Number

[3055319-82-6]

UNSPSC

12352005

Target

PI3K; Ras

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

COC1=CC(C2=C(Cl)C=CC=C2)=C(S(N3CC[C@](C(N[C@@H](/C=C\S(C)(=O)=O)C)=O)(F)C[C@H]3C)(=O)=O)C=C1

Molecular Formula

C25H30ClFN2O6S2

Molecular Weight

573.10

References & Citations

[1]Klebba JE, et al. Covalent inhibitors of the RAS binding domain of PI3Kα impair tumor growth driven by RAS and HER2. bioRxiv [Preprint]. 2024 Dec 20:2024.12.17.629001. PMCID: PMC11703231.1.