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Gartisertib-d8

Cat.No.:HY-136270S

CASNo.:1792214-00-6

Synonyms:VX-803-d;M4344-d;ATRinhibitor2-d

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分⼦式:C₂₅H₂₁D₈F₂N₉O₃

分⼦量:549.6

作⽤靶点:Isotope-LabeledCompounds;ATM/ATR

作⽤通路:Others;CellCycle/DNADamage;PI3K/Akt/mTOR

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性Gartisertib-d8(VX-803-d8)是氘代标记的Gartisertib(HY-136270)。Gartisertib(VX-803)是⼀种ATP竞争性

的，具有⼝服活性的，选择性的ATR抑制剂，Ki150pM。Gartisertib抑制ATR驱动的磷酸化检查点激酶-1

(Chk1)磷酸化,IC50值为8nM。具有抗肿瘤活性。

体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,

largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattention

becauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs.

REFERENCES

[1].FrankT.Zenke,etal.A