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Description: Potent covalent inhibitor of the RAS domain of the PI3K/p110α interaction
Chemical Name: 5-((1R,2S,5S)-2-(2-Chloro-3-fluorophenyl)-3-azabicyclo[3.1.0]hexan-3-yl)-N-((R,E)-4-(methylsulfonyl)but-3-en-2-yl)pyrazine-2-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for VVD 844
VVD 844 is a potent inhibitor of the PI3K/p110α interaction (IC50 = 4 nM) and the phosphorylated-Ser473-AKT (pAKT) pathway (IC50 = 11 nM). It covalently binds cysteine 242 in the RAS domain of PI3K/p110α and blocks RAS activation of PI3Kα activity in vitro.
In vivo, VVD 844 slows growth of RAS mutant tumors and human epidermal growth factor receptor 2 (HER2)-overexpressing tumors, without causing hyperglycemia. Exhibits synergistic effects with Sotorasib (Cat. No. 7713) and Adagrasib (Cat. No. 7488). VVD 844 is orally bioavailable.
Licensing Information
Sold with permission from Vividion Therapeutics
Technical Data for VVD 844
| M. Wt | 464.94 |
| Formula | C21H22ClFN4O3S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 3080226-63-4 |
| PubChem ID | 176259150 |
| InChI Key | WLYRECBTSICUGW-DATNFHAOSA-N |
| Smiles | ClC1=C(C=CC=C1F)[C@@H]2[C@@]3([H])[C@](CN2C4=NC=C(C(N[C@H](C)/C=C/S(C)(=O)=O)=O)N=C4)([H])C3 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for VVD 844
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.49 | 100 | |
| ethanol | 46.49 | 100 |
Preparing Stock Solutions for VVD 844
The following data is based on the product molecular weight 464.94. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.15 mL | 10.75 mL | 21.51 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.3 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets for VVD 844
References for VVD 844
References are publications that support the biological activity of the product.
Klebba et al (2025) Covalent inhibitors of the PI3Kα RAS binding domain impair tumor growth driven by RAS and HER2. Science 390 702 PMID: 41066541
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Citations for VVD 844
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
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Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.
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In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Pathways for VVD 844
Akt Signaling Pathway
The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.