VVD 844
Tocris Bioscience, part of Bio-Techne | Catalog # 8952
Potent covalent inhibitor of the RAS domain of the PI3K/p110α interaction
Key Product Details
Description
Potent covalent inhibitor of the RAS domain of the PI3K/p110α interaction
Product Description
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 TherapeuticsProduct Specifications
Molecular Weight
464.94
Formula
C21H22ClFN4O3S
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 | 4.30 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Klebba Covalent inhibitors of the PI3Kα RAS binding domain impair tumor growth driven by RAS and HER2. Science 2025 PMID: 41066541
Product Specific Notices for VVD 844
For research use only
Loading...
Loading...