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VVD 844

Cat. No. 8952 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent covalent inhibitor of the RAS domain of the PI3K/p110α interaction
化学名： 5-((1R,2S,5S)-2-(2-Chloro-3-fluorophenyl)-3-azabicyclo[3.1.0]hexan-3-yl)-N-((R,E)-4-(methylsulfonyl)but-3-en-2-yl)pyrazine-2-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (4)
通路 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for VVD 844

VVD 844 is a potent inhibitor of the PI3K/p110α interaction (IC50 = 4 nM) and the phosphorylated-Ser473-AKT (pAKT) pathway (IC50 = 11 nM). It covalently binds cysteine 242 in the RAS domain of PI3K/p110α and blocks RAS activation of PI3Kα activity in vitro.

In vivo, VVD 844 slows growth of RAS mutant tumors and human epidermal growth factor receptor 2 (HER2)-overexpressing tumors, without causing hyperglycemia. Exhibits synergistic effects with Sotorasib (Cat. No. 7713) and Adagrasib (Cat. No. 7488). VVD 844 is orally bioavailable.

许可信息

Sold with permission from Vividion Therapeutics

技术数据 for VVD 844

分子量 464.94
公式 C21H22ClFN4O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 3080226-63-4
PubChem ID 176259150
InChI Key WLYRECBTSICUGW-DATNFHAOSA-N
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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for VVD 844

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.49 100
ethanol 46.49 100

制备储备液 for VVD 844

以下数据基于产品分子量 464.94。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.15 mL 10.75 mL 21.51 mL
5 mM 0.43 mL 2.15 mL 4.3 mL
10 mM 0.22 mL 1.08 mL 2.15 mL
50 mM 0.04 mL 0.22 mL 0.43 mL

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参考文献 for VVD 844

参考文献是支持产品生物活性的出版物。

Klebba et al (2025) Covalent inhibitors of the PI3Kα RAS binding domain impair tumor growth driven by RAS and HER2. Science 390 702 PMID: 41066541

If you know of a relevant reference for VVD 844, please let us know.

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关键词: VVD 844, VVD 844 supplier, VVD844, potent, covalent, inhibitor, inhibits, binds, blocks, RAS, domain, PI3K, PI3K/p110α, p110-alpha, p110a, interaction, mutant, tumors, human, epidermal, growth, factor, receptor, 2, HER2, overexpressing, sotorasib, adagrasib, orally, bioavailable, Ras, GTPases, 8952, Tocris Bioscience

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该领域的文献

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*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。

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Pathways for VVD 844

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.
MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.