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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 3080226-63-4
- Formel: C21H22ClFN4O3S
- Molecular Weight:464.94
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
|
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.
-
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).
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.
Chemical Information
-
CAS. Nr. 3080226-63-4
-
Molecular Weight 464.94
-
Formel C21H22ClFN4O3S
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
VVD-844 Related Classifications
HY-183741 Related Classifications
Powered by Bioz