1. PI3K/Akt/mTOR
  2. PI3K Akt
  3. VVD-484

VVD-484 is a PI3K p110α inhibitor with an IC50 of 0.59 μM against human targets.,VVD-484, classified as a "silent ligand", forms a covalent bond with Cys242 of PI3K p110α without disrupting the p110α-KRASG12C interaction. VVD-484 inhibits phosphorylation (S473) of AKT via a RAS-independent pathway. VVD-484 can be used in the research of HER2-overexpressing cancers.

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VVD-484

VVD-484 Chemical Structure

CAS No. : 3055745-21-3

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Description

VVD-484 is a PI3K p110α inhibitor with an IC50 of 0.59 μM against human targets.,VVD-484, classified as a "silent ligand", forms a covalent bond with Cys242 of PI3K p110α without disrupting the p110α-KRASG12C interaction. VVD-484 inhibits phosphorylation (S473) of AKT via a RAS-independent pathway. VVD-484 can be used in the research of HER2-overexpressing cancers[1].

In Vitro

VVD-484 (2 h) potently inhibits PI3K/AKT signaling in N87 HER2-overexpressing gastric cancer cells, despite not disrupting the RAS-p110α interaction[1].
VVD-484 does not disrupt the interaction between p110α and alternate RAS isoforms (RRAS, ERAS, MRAS, RRAS2) in H358 cell lysates[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

466.95

Formula

C24H29ClF2N2O3

CAS No.
SMILES

FC1(C2(CCN(C1)C([C@H]3[C@@H](C4=C(C=CC=C4)Cl)CC(C)(OC3)C)=O)CN(C2)C(C=C)=O)F

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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VVD-484
Cat. No.:
HY-185205
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