JMF4073-生命科学试剂-MCE.pdf

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Inhibitors•ScreeningLibraries•Proteins

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JMF4073

Cat.No.:HY-162698

CASNo.:1927930-61-7

分⼦式:C₁₈H₂₂FN₃O₄S

分⼦量:395.45

作⽤靶点:ThymidylateSynthase

作⽤通路:Apoptosis

储存⽅式:Pleasestoretheproductundertherecommendedconditionsin

theCertificateofAnalysis.

BIOLOGICALACTIVITY

⽣物活性JMF4073是⼀种胸苷酸(TMP)和胞苷酸(CMP)激酶抑制剂，IC50分别为0.16μM和0.17μM。JMF4073在

体外和体内消除野⽣型(WT)-Bcr-Abl转化的髓系细胞。

体外研究WT-Bcr-AblcellsarehighlysusceptibletoJMF4073withGI500.67μMascomparedto1.5 μMand4.2 μM

forT315I-Bcr-Abl-32Danduntransformed32Dcells,respectively.Thelevelsofoveralltyrosine

phosphorylationinthesecellswereunaffectedbyJMF4073treatment[1].

体内研究JMF4073(5 mg/kg;ip;daily;for14days)inhibitswhitebloodcountsinWT-Bcr-Abl-32Dbearingmice.

Moreover,JMF4073prolongsthesurvivalofleukemiamice[1].

AnimalModel:C3H/HeNCrNarlmiceinjectedwithWT-Bcr-Abl-32Dchronicmyeloidleukemia(CML)

cells[1]

Dosage:5 mg/kg

Administration:Intraperitonealinjection;daily;for14days

Result:Prolongedthesurvivalofleukemiamice.

REFERENCES