Chemical Structure : VVD-699
CAS No.:
3055319-82-6
VVD-699
(VVD699)
Catalog No.: PC-23785Not For Human Use, Lab Use Only.
VVD-699 is a specific, covalent inhibitor of RAS binding domain of PI3Kα (p110α RBD), disrupts the RAS-p110α interaction, binds covalently to Cys242 in p110α RBD and blocks the ability of RAS to activate PI3K activity.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
VVD-699 is a specific, covalent inhibitor of RAS binding domain of PI3Kα (p110α RBD), disrupts the RAS-p110α interaction, binds covalently to Cys242 in p110α RBD and blocks the ability of RAS to activate PI3K activity.
VVD-699 shows no impact on p110α lipid kinase activity in biochemical assays.
VVD-699 inhibited pAKT in KRASG12S A549 cells, and this effect was lost in isogenic p110α C242S knock-in A549 cells, blocked downstream pathway activation across a wide range of cancer relevant RAS and p110α mutations.
VVD-699 inhibits HER2 activity through an H/K/N-RAS independent mechanism in KRAS hyperactive cell lines.
VVD-699 (100 mg/kg, oral) inhibits tumor growth without impacting glucose homeostasis in mice bearing FaDu xenografts (KRASamp), sensitizes tumors to KRASG12C Inhibition.
Physicochemical Properties
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M.Wt
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573.09
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Formula
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C25H30ClFN2O6S2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(2R,4S)-1-((2'-chloro-5-methoxy-[1,1'-biphenyl]-2-yl)sulfonyl)-4-fluoro-2-methyl-N-((R,Z)-4-(methylsulfonyl)but-3-en-2-yl)piperidine-4-carboxamide
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References
1. Klebba JE, et al. bioRxiv [Preprint]. 2024 Dec 20:2024.12.17.629001.
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