Crotonoside-Isoguanosine-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECrotonosideCat. No.: HY-N0071CAS No.: 1818-71-9Synonyms: Isoguanosine分式: CHNO分量: 283.24作靶點(diǎn): FLT3; HDAC作通路: Protein Tyrosine Kinase/RTK; Cell Cycle/DNA Damage;Epigenetics儲存式: Please store the product under the recommended conditi

2、ons inthe COA.BIOLOGICAL ACTIVITY物活性 Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6,exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising newlead compound for the treatment of AML 1.IC50 & Target FLT3

3、 HDAC3 HDAC6體外研究Crotonoside (0-200 M;) selectively inhibits the viability of AML cell line MV4-11, MOLM-13 (with FLT3-ITDmutant) and KG-1 (without FLT3-ITD mutant) in a dose-dependent manner with an IC50 of 11.6 M, 12.7 Mand 17.2 M, respectively 1.Crotonoside (0-100M; 7 hours) inhibits the phosphory

4、lation of FLT3 Erk1/2,Akt/mTOR and STAT5 is strongly inhibited by crotonoside at higher concentration of 12.5 M in aconcentration-dependent manner 1.Crotonoside (0-100 M; 12 hours) exhibits a dose-dependent increasein the percentage of G0/G1 phase and a dose-dependent decrease in the percentage of G

5、2/M and S phasescells 1. Crotonoside (0-100 M; 24 hours) leads to concentration-dependent changes in the number ofapoptotic MV4-11 cells, results in a dose-dependent decrease in the level of pro-caspase-3 and a dose-dependent increase in the level of the cleaved caspase-3 fragments 1.Cell Viability

6、Assay 1Cell Line: AML cell line MV4-11, MOLM-13 and KG-1 cellsConcentration: 0-200 M1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEIncubation Time: 72 hoursResult: Inhibited AML cells growth than other cell lines tested.Western Blot Analysis 1Cell Line: MV4-11 cellsConcentration: 0 M, 12.5 M, 25 M

7、, 50 MIncubation Time: 7 hoursResult: Inhibited AML cells growth than other cell lines tested.Cell Cycle Analysis 1Cell Line: MV4-11 cellsConcentration: 0 M, 12.5 M, 25 M, 50 MIncubation Time: 12 hoursResult: Induced cell cycle arrest in G0/G1.Apoptosis Analysis 1Cell Line: MV4-11 cellsConcentration

8、: 0 M, 12.5 M, 25 M, 50 MIncubation Time: 24 hoursResult: Induced MV4-11 cell apoptosis.體內(nèi)研究 Crotonoside(intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily) induces a significantantitumor activity and inhibited xenograft tumor progress as compared to treatment with vehicle 1.A

9、nimal Model: NOD-SCID mice with MV4-11 cells 1Dosage: 70 mg/kg, 35 mg/kgAdministration: Intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once dailyResult: Produced significant AML tumor inhibition rates of 93.5% at 70 mg/kg.REFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Li YZ,et al. Crotonoside exhibits selective post-inhibition effect in AML cells via inhibition of FLT3 and HDAC3/6. Oncotarget. 2017 Sep8;8(61):103087-103099.McePdfHeightCaution: Product has not been fully validated f