ERGi-USU-6 (mesylate) is an ERGi-USU-6 salt derivative that is a new selective inhibitor of ERG positive prostate cancer ( IC50 = 0.089 μM).
分子量
338.38
Formula
C14H18N4O4S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Eldhose B, et al. New Selective Inhibitors of ERG Positive Prostate Cancer: ERGi-USU-6 Salt Derivatives. ACS Med Chem Lett. 2021 Oct 19;12(11):1703-1709.
ERGi-USU-6 (mesylate) is an ERGi-USU-6 salt derivative that is a new selective inhibitor of ERG positive prostate cancer ( IC50 = 0.089 μM).
分子量
338.38
Formula
C14H18N4O4S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Eldhose B, et al. New Selective Inhibitors of ERG Positive Prostate Cancer: ERGi-USU-6 Salt Derivatives. ACS Med Chem Lett. 2021 Oct 19;12(11):1703-1709.
ERGi-USU-6 (mesylate) is an ERGi-USU-6 salt derivative that is a new selective inhibitor of ERG positive prostate cancer ( IC50 = 0.089 μM).
分子量
338.38
Formula
C14H18N4O4S
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Eldhose B, et al. New Selective Inhibitors of ERG Positive Prostate Cancer: ERGi-USU-6 Salt Derivatives. ACS Med Chem Lett. 2021 Oct 19;12(11):1703-1709.
NSC139021 (ERGi-USU) is a highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM.
IC50 & Target
IC50: 30 to 400 nM (ERG-positive cancer cells)[1]
体外研究 (In Vitro)
NSC139021 selectively inhibits growth of ERGpositive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines. The IC50 of NSC139021 for cell growth inhibition of responsive cell lines range between 30 nM to 400 nM. Combination of NSC139021 with enzalutamide shows additive effects in inhibiting growth of VCaP cells. A screen of kinases reveal that NSC139021 directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induces ribosomal stress signature[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
NSC139021 treatment inhibits growth of ERG-positive VCaP tumor xenografts with no apparent toxicity. Significant (P<0.05, P<0.005) inhibition of tumor growth is noted at day 26 in treatment groups indicating 44% (100 mg/kg) and 65% (150 mg/kg) reduction of tumor burden. At 100 mg/kg and 150 mg/kg, no apparent toxicity including weight loss, lethargy, diarrhea, loss of appetite, respiratory distress, or overall drug related toxicity is observed. [1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
255.30
Formula
C13H9N3OS
CAS 号
1147-56-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Mohamed AA, et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth. Cancer Res. 2018 Apr 30. pii: canres.2949.2017.
Cell Assay [1]
To assess cell growth, To evaluate the ERG selectivity of the NSC139021, a panel of the following cell lines are assessed: ERG positive tumor cell lines (prostate cancer: VCaP; colon cancer: COLO320; leukemia: KG-1, MOLT-4; ERG negative prostate cancer cell lines (LNCaP, LAPC4, MDA PCa2b); normal prostate epithelium derived cell lines (BPH-1, RWPE-1); and primary endothelium derived cells (HUVEC). Monolayer of adherent cells are grown in their respective medium for 48 h followed by treatment with indicated dosage and time for the small molecule inhibitor NSC139021. Medium is replaced every 24 h containing the same concentration of the small molecule compound. Cells are counted by using trypan blue exclusion method. Cell morphology is documented by photography in all indicated time points. IC50 is calculated using GraphPad Prism 6 software[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [1]
Mice[1]
The VCaP prostate cancer cells are injected into lower right dorsal flank of the male athymic nude mice (6-8 weeks old and weighing 27 to 30g). when tumors are palpable, mice are randomly separated into 2 experimental groups and into one control group of 6 mice in each group. In the treatment groups mice are injected intraperitoneally (I.P) with 100 mg/kg of NSC139021 or 150 mg/kg of NSC139021 while the control group are injected with vehicle (1:1[v/v], DMSO/PEG300) only. Growth in tumor volume is recorded weekly by using digital calipers and tumor volumes are calculated[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Mohamed AA, et al. Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth. Cancer Res. 2018 Apr 30. pii: canres.2949.2017.