VVD-699 | p110α RBD inhibitor | Probechem Biochemicals

Chemical Structure : VVD-699

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VVD-699 (VVD699)

货号: PC-23785Not For Human Use, Lab Use Only.

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250 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	573.09
分子式	C25H30ClFN2O6S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. Klebba JE, et al. bioRxiv [Preprint]. 2024 Dec 20:2024.12.17.629001.

VVD-699 (VVD699)

生物&药学活性

物理化学性质&存储条件

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VVD-699 (VVD699)

生物&药学活性

物理化学性质&存储条件

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