Bioactivity | UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity[1]. | ||||||||||||
Invitro | UC-514321 increases apoptosis in AML cells not in normal HSPCs[1].UC-514321 (0-500 nM, 48 h) inhibits AML cells viability TET1-signaling dependently[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
In Vivo | UC-514321 (2.5 mg/kg, ip, once per day, for 10 days) exhibits more potent anti-tumor activity than NSC370284 in AML mice models[1]. Animal Model: | ||||||||||||
Name | UC-514321 | ||||||||||||
CAS | 299420-83-0 | ||||||||||||
Formula | C26H35NO5 | ||||||||||||
Molar Mass | 441.56 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Jiang X, et al. Targeted inhibition of STAT/TET1 axis as a therapeutic strategy for acute myeloid leukemia. Nat Commun. 2017 Dec 13;8(1):2099. |