2. PI3K/Akt/mTOR
  3. PI3K Akt
  4. VVD-844

VVD-844 is an orally active covalent inhibitor of PI3Kα inhibitor. VVD-844 covalently binds to Cys242 in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2-overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers.

For research use only. We do not sell to patients.

VVD-844

VVD-844 Chemical Structure

CAS No. : 3080226-63-4

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VVD-844 Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

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Description

VVD-844 is an orally active covalent inhibitor of PI3Kα inhibitor. VVD-844 covalently binds to Cys242 in the RAS binding domain of p110α, blocking RAS-p110α interaction and inhibiting PI3Kα activity. VVD-844 inhibits PI3Kα signaling activation in HER2-overexpressing cells via a RAS-independent mechanism. VVD-844 suppresses tumor growth in mouse. VVD-844 can be used for the research of cancers[1].

IC50 & Target[1]

PI3Kα

 

In Vitro

VVD-844 (10 nM; 2-24 h) inhibits PI3K/AKT signaling in KPAR (KRASG12C) mouse lung cancer cells[1].

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

VVD-844 Related Antibodies

Western Blot Analysis[1]

Cell Line: KPAR (KRASG12C) mouse lung cancer cells
Concentration: 10 nM
Incubation Time: 2; 24 h
Result: Decreased pAKT (S473) levels.
Decreased pERK1/2 levels when combined with Adagrasib (HY-130149).
In Vivo

VVD-844 (10 mg/kg; p.o.; b.i.d.) inhibits tumor growth in mouse CTG3196 and CR2528 PDX models[1].

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

Animal Model: Nu/Nu mice (6-8
weeks) subcutaneously inoculated with CTG3196 tumor[1]
Dosage: 10 mg/kg
Administration: p.o.; b.i.d.
Result: Inhibited tumor growth compared to control.
Animal Model: Nu/Nu mice (6-8
weeks) subcutaneously inoculated with CR2528 tumor[1]
Dosage: 10 mg/kg
Administration: p.o.; b.i.d.
Result: Inhibited tumor growth compared to control.
Molecular Weight

464.94

Formula

C21H22ClFN4O3S
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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VVD-844 Related Classifications

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Help & FAQs
  • 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.

Keywords:

VVD-8443080226-63-4VVD844VVD 844PI3KAktPhosphoinositide 3-kinasePKBProtein kinase Bp110αKRAS mutantEGFR mutantRAS binding domainHER2-overexpressing cellsCys242patient-derived xenograft modelsKPAR mouse lung cancer cellsKRAS-p110α co-mutantHEK293T cell lysatesInhibitorinhibitorinhibit

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