VVD 844

Tocris Bioscience | Catalog # 8952

Potent covalent inhibitor of the RAS domain of the PI3K/p110α interaction
Tocris Bioscience
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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 Therapeutics

Product Specifications for VVD 844

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.

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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.

Select a batch to recalculate based on the batch molecular weight:

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

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Background References

References are publications that support the biological activity of the product.

Product Documents for VVD 844

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for VVD 844

For research use only

Related Research Areas

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