VVD-844
VVD-844 is an orally active covalent inhibitor of PI3Kα, which inhibits Pl3Kα/p110α interaction with an IC50 of 4 nM. 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.
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- No. CAS: 3080226-63-4
- Fòrmula: C21H22ClFN4O3S
- Peso molecular:464.94
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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PI3Kα |
VVD-844 (10 nM; 2-24 h) inhibits PI3K/AKT signaling in KPAR (KRASG12C) mouse lung cancer cells[1].
VVD-844 inhibits phosphorylated-Ser473-AKT (pAKT pathway with an lC50 of 11 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KPAR (KRASG12C) mouse lung cancer cells
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Concentration:10 nM
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Incubation Time:2; 24 h
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Result:Decreased pAKT (S473) levels.
Decreased pERK1/2 levels when combined with Adagrasib (HY-130149).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nu/Nu mice (6-8
weeks) subcutaneously inoculated with CTG3196 tumor[1] -
Dosage:10 mg/kg
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Administration:p.o.; b.i.d.
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Result:Inhibited tumor growth compared to control.
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Animal Model:Nu/Nu mice (6-8
weeks) subcutaneously inoculated with CR2528 tumor[1] -
Dosage:10 mg/kg
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Administration:p.o.; b.i.d.
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Result:Inhibited tumor growth compared to control.
Chemical Information
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No. CAS 3080226-63-4
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Peso molecular 464.94
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Fòrmula C21H22ClFN4O3S
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VVD-844 Related Classifications
HY-183741 Related Classifications
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