| Bioactivity | NSC139021 (ERGi-USU) is a highly selective inhibitor for the growth of ERG-positive cancer cells with IC50s ranging from 30 to 400 nM. | ||||||||||||
| Target | IC50: 30 to 400 nM (ERG-positive cancer cells) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| 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]. | ||||||||||||
| Name | NSC139021 | ||||||||||||
| CAS | 1147-56-4 | ||||||||||||
| Formula | C13H9N3OS | ||||||||||||
| Molar Mass | 255.30 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |