| Bioactivity | NSC-370284 is a selective inhibitor of ten-eleven translocation 1 (TET1) and 5-hydroxymethylcytosine (5hmC). NSC-370284 significantly inhibits the level of TET1 expression via targets STAT3/5[1]. | ||||||||||||
| Invitro | NSC-370284 (0-500 nM；24 h 或 48 h) 通过靶向 STAT3/5 抑制 MONOMAC-6、THP-1、KOCL-48 和 KASUMI-1 急性髓系白血病 (AML) 细胞活力。NSC-370284 显著下调 TET1 转录水平[1]。 Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | NSC-370284 (2.5 mg/kg；腹腔注射，每天一次，持续 10 天) 改善了 MLL-AF9 急性髓系白血病 (AML) 小鼠模型外周血 (PB)、骨髓 (BM)、脾和肝组织的病理形态学[1]。 Animal Model: | ||||||||||||
| Name | NSC-370284 | ||||||||||||
| CAS | 116409-29-1 | ||||||||||||
| Formula | C21H25NO6 | ||||||||||||
| Molar Mass | 387.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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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. |